DOCSLIB.ORG

Antibacterial Or Bactericide Comprising 2-Aminothiazole Derivative and Salts Thereof

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Antibacterial Or Bactericide Comprising 2-Aminothiazole Derivative and Salts Thereof E-™ II 1 1 INI II IMI 1 1 II II I Mil II I II European Patent Office Office europeen des brevets (11) EP 0 790 057 A1 (12) EUROPEAN PATENT APPLICATION published in accordance with Art. 158(3) EPC (43) Date of publication: (51) Int. CI.6: A61 K 31/425, C07D 277/40, 20.08.1997 Bulletin 1997/34 C07D 277/42, C07D 277/44, (21) Application number: 95938022.1 C07D 41 7/04 (22) Date of filing: 16.11.1995 (86) International application number: PCT/JP95/02347 (87) International publication number: WO 96/16650 (06.06.1996 Gazette 1996/26) (84) Designated Contracting States: • YOSHIDA, Toshio CH DE FR GB IE LI Hisamitsu Pharmaceutical Co., Inc. Saga 841 (JP) (30) Priority: 29.11.1994 JP 317737/94 . ITOYAMA, Toshio, 22.1 2.1 994 JP 335388/94 Tsukuba Laboratory, 1-chome Tsukuba-shi, Ibaraki 305 (JP) (71) Applicant: . TANIGUCHI, Yasuaki HISAMITSU PHARMACEUTICAL CO. INC. Hisamitsu Pharm Co., Inc. Tosu-shi Saga 841 (JP) Saga 841 (jP) (72) Inventors: (74) Representative: Modiano, Guido, Dr.-lng. et al • HASHIGUCHI, Terushi Modiano, Josif, Pisanty & Staub, Hisamitsu Pharmac. Co., Inc. Baaderstrasse 3 Tosu-shi Saga 841 (JP) 80469 Munchen (DE) (54) ANTIBACTERIAL OR BACTERICIDE COMPRISING 2-AMINOTHIAZOLE DERIVATIVE AND SALTS THEREOF (57) An antibacterial or bactericide comprising a 2- aminothiazole derivative represented by general for- mula (I) or a salt thereof, wherein R1 and R2 represent each hydrogen, halogeno, lower alkyl, lower cycloalkyl, (un)substituted phenyl, thiophene, benzoyl, benzoylme- thyl, optionally substituted benzyl, p-pivoloyloxyphenyl, - COOR3 (wherein R3 represents hydrogen or lower alkyl) or -CH2COOR4 (wherein R4 represents hydrogen, lower alkyl or optionally substituted benzyl); and A1 and A2 represent each hydrogen, lower alkanesulfonyl, hal- ogenated lower alkanesulfonyl, optionally substituted phenyl, substituted benzoyl, substituted benzyl, (un)substituted benzenesulfonyl, (un)substituted lower alkanoyl, amidino, -CO-R5 (wherein R5 represents lower alkyl, optionally substituted phenyl, -(CH2)m- ,,_ COOH (wherein m represents an integer of 1 to 5), - <^ (CH2)n-NH-R6 (wherein n represents an integer of 1 to and ^ 5, R6 represents hydrogen, tert-butoxycarbonyl or If) benzyloxycarbonyl) or -(CH2)Q-R7 (wherein Q repre- O sents an integer of 0 to 5, and R7 represents lower O alkoxy, optionally substituted phenyl, optionally substi- tuted pyridyl or cyclic amino), or A1 and A2 are com- bined with each other to represent cyclic amino. Q_ LU Printed by Rank Xerox (UK) Business Services 2.14.12/3.4 EP 0 790 057 A1 Description Technical Field 5 This invention relates to an antibacterial preparation or a bactericide, comprising a 2-aminothiazole derivative and a salt thereof. The term "bactericide" used herein connotes disinfectants. Background Art 10 Prior art will be described. At the outset, thiazoles having a trifluoromethanesulfonylamino group at the 2-position are described in U.S. Patent Nos. 3,923,810 and 3,923,811. Japanese Pat. Appln. Laid-Open Gazettes Nos. Sho 64- 40474 (40474/89) and Sho 64-75475 (75475/89) describe thiazole derivatives having anti-inflammatory action and analgesic action. Phenyl pivalate derivatives are described as an elastase inhibitor in U.S. Patent No. 4,801,610 and Japanese Pat. Appln. Laid-Open Gazette No. Hei 3-20253 (20253/91). Further, the compounds or part of the com- 15 pounds of this invention are described also in Japanese Pat. Appln. Laid-Open Gazettes Nos. Hei 3-173876 (173876/91) and Hei 5-70446 (70446/93). However, the antibacterial action or bactericidal action of the compounds of this invention is not disclosed at all, nor is it suggested. Disclosure of the Invention 20 An object of this invention is to provide an antibacterial preparation or a bactericide each of which comprises a com- prising a 2-aminothiazole derivative and a salt thereof, exhibits a tendency of low bacterial tolerance thereto and low toxicity and has antibacterial activity or bactericidal activity, and the object is also to provide a pharmaceutical compris- ing the antibacterial preparation or the bactericide. 25 This invention relates to a novel antibacterial agent or bactericide comprising 2-aminothiazole derivatives and salts thereof as effective ingredients. More specifically, this invention relates to 2-aminothiazole derivatives represented by the following general formula (I) and their salts useful as pharmaceutical preparations: 30 wherein R1 and R2 each represent a hydrogen atom; a halogen atom; a lower alkyl, lower cycloalkyl, substituted or unsubstituted phenyl, thiophene, benzoyl, benzoylmethyl, benzyl or substituted benzyl or p-pivaloyloxyphenyl group; 40 -COOR3 wherein R3 is a hydrogen atom, a lower alkyl group; and -CH2COOR4 wherein R4 is a hydrogen atom or a lower alkyl, benzyl or substituted benzyl group; and A1 and A2 each represent a hydrogen atom; a lower alkanesulfonyl, halo lower alkanesulfonyl, phenyl or substituted phenyl, substituted benzoyl, substituted benzyl, substituted or unsub- stituted benzenesulfonyl, substituted or unsubstituted lower alkanoyl or amidino group; -CO-R5 wherein R5 is a lower alkyl, phenyl or substituted phenyl group, -(CH2)m-COOH wherein m is an integer of 1 to 5, or -(CH2)n-NH-R6 wherein 45 n is an integer of 1 to 5 and R6 is a hydrogen atom or a tert-butoxycarbonyl, benzyloxycarbonyl group; and -(CH2)Q-R7 wherein Q is an integer of 0 to 5 and R7 is a lower alkoxy, phenyl or substituted phenyl, pyridyl or substituted pyridyl, cyclic amino group; or A1 and A2 may combine with each other to form a cyclic amino group. The general formula (I) will be described in detail. The halogen atoms include fluorine, chlorine, bromine and iodine. The lower alkyl groups include C1 - C8 alkyl groups such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl so and tert-butyl groups. The lower cycloalkyl groups include C3 - C6 cycloalkyl groups such as cyclopropyl, cyclobutyl, cyclopentane and cyclohexane groups. The lower alkoxy groups include C1 - C6 alkoxy groups such as methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, iso-butoxy and tert-butoxy groups. The lower alkanesulfonyl groups include C1 - C4 alkanesulfonyl groups such as methanesulfonyl, ethanesulfonyl, n-propanesulfonyl, iso-propanesulfonyl n-butanesulfo- nyl groups, iso-butanesulfonyl and tert-butanesulfonyl groups. The halo lower alkanesulfonyl group is a halo lower 55 alkanesulfonyl group substituted by one or a plurality of halogen atoms, and the substituted alkanesulfonyl groups include mono-, di- or tri-fluoromethanesulfonyl, chloromethanesulfonyl, bromomethanesulfonyl, fluoroethanesulfonyl, chloroethanesulfonyl and bromoethanesulfonyl groups. The substituted or unsubstituted lower alkanoyl group is a C1 - C4 halo lower alkanoyl group substituted by an amino group or one to three halogen atoms, and the alkanoyl groups so substituted or not include aminoacetyl, monofluoroacetyl, difluoroacetyl, trifluoroacetyl, monochloroacetyl, dichloro- 2 EP 0 790 057 A1 acetyl, trichloroacetyl, monofluoropropionyl, difluoropropionyl and trifluoropropionyl groups. The lower alkanoyloxy groups include Ci - C6 alkanoyloxy groups such as acetyl, propionyl, butyryl, valeryl and pivaloyl groups. The cyclic amino groups include 5-or 6-membered cyclic amino groups optionally containing a nitrogen or oxygen atom, such as piperidino, pyrrolidine, morpholino, piperazino and pipecolino groups (the cyclic amino groups may be further substi- 5 tuted by a halogen atom, a lower alkyl group or the like). The substituents in the substituted phenyl, substituted benzyl, substituted pyridyl groups and substituted benzenesulfonyl groups refer to those substituted at their optional one to three positions by lower alkyl groups, halogen atoms, hydroxyl groups, nitro groups, phenyl groups, trifluoromethyl groups, lower alkoxy groups, halo lower alkoxy groups substituted by one or a plurality of halogen atoms, lower alkanesulfonyl groups, halo lower alkanesulfonyl groups, amino groups, Ci - C6 di-lower-alkylamino groups such as 10 dimethylamino, diethylamino, di-n-propylamino and di-n-butylamino groups, Ci - C6 lower alkylsulphenyl groups such as methylsulphenyl, ethylsulphenyl, n-propylsulphenyl, iso-propylsulphenyl, n-butylsulphenyl and tert-butylsulphenyl groups, C2 - C6 lower alkanoylamino groups such as acetylamino, propionylamino, butyrylamino, iso-butyrylamino, valerylamino and pivaloylamino groups, lower alkanoyloxy groups, Ci -C4 lower mercapto groups such as methylthio, ethylthio, n-propylthio, iso-propylthio, n-butylthio, iso-butylthio and tert-butylthio groups, hydroxyl groups, acetic groups, 15 Ci - C4 acetic ester groups such as methyl acetate, ethyl acetate, propyl acetate and butyl acetate groups, Ci - C4 gly- colic ester groups such as methyl glycolate, ethyl glycolate, propyl glycolate and butyl glycolate groups, or the like; and also refer to -COOR4 and -CH2COOR4 wherein R4 is as defined above. Pharmaceutically acceptable salts thereof include, but are not limited to, inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid and phosphoric acid; organic acids such as maleic acid, fumaric acid, oxalic acid, succinic acid, 20 malonic acid, lactic acid, citric acid, methanesulfonic acid, benzenesulfonic acid and acetic acid; inorganic salts, for example, alkali metal salts such as lithium salts, sodium salts and potassium salts, alkaline earth metal salts such as calcium salts and magnesium salts, and ammonium salts; and organic salts such as triethylamine salts, ethanolamine salts, triethanolamine salts and dicyclohexylamine
Load more

Recommended publications
  • A Review on Antimicrobial Resistance in Developing Countries
    mac har olo P gy : & O y r p t e s i n Biochemistry & Pharmacology: Open A m c e c h e c Ravalli, et al. Biochem Pharmacol 2015, 4:2 s o i s B Access DOI: 10.4172/2167-0501.1000r001 ISSN: 2167-0501 Review Open Access A Review on Antimicrobial Resistance in Developing Countries Ravalli R1*, NavaJyothi CH2, Sushma B3 and Amala Reddy J4 1Deparment of Pharmaceutical Sciences, Andhra University, Vishakapatnam, India 2University College of Technology, Osmania University, Hyderabad, India 3Deparment of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad, India 4Deparment of Pharmaceutical Sciences, Osmania University, Hyderabad, India *Corresponding author: Ravalli R, Deparment of Pharmaceutical Sciences, Andhra University, Vishakapatnam, India, Tel: + 0437-869-033; E-mail: [email protected] Received date: April 13, 2015; Accepted date: April 14, 2015; Published date: April 21, 2015 Copyright: © 2015 Ravalli Remella. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestri cted use, distribution, and reproduction in any medium, provided the original author and source are credited. Availability of Antimicrobial Drugs isolates were proof against Principen, Co-trimoxazole, and bactericide, and 14-40% were given with Mecillinam [6]. This was associate degree Although foremost potent and recently developed antimicrobial outsized increase over the half resistant isolates notable in 1991, before medicine are offered throughout the globe, in developing countries the drug was wide on the market. Throughout infectious disease their use is confined to people who are flush enough to afford them. In epidemics the organism has the flexibleness to develop increasing tertiary referral hospitals like the Kenyatta National Hospital in resistance, typically by acquisition of plasmids.
    [Show full text]
  • Mankocide® Fungicide/Bactericide
    SAFETY DATA SHEET Issue Date 25-Feb-2017 Revision Date 25-Feb-2017 Version 1 1. IDENTIFICATION Product identifier Product Name ManKocide® Fungicide/Bactericide Other means of identification Product Code 91411-7 Synonyms ManKocide DF, B12262770 Registration Number(s) 91411-7-70051 Recommended use of the chemical and restrictions on use Recommended Use Fungicide Bactericide Uses advised against No information available Details of the supplier of the safety data sheet Manufacturer Address Distributed by: Kocide LLC Certis U.S.A. L.L.C. 9145 Guilford Road, Suite 175 9145 Guilford Road, Suite 175 Columbia, MD 21046 Columbia, MD 21046 USA USA Website: www.kocide.com www.certisusa.com Emergency telephone number Company Phone Number Certis USA +1 301-604-7340 Emergency Telephone ChemTel, Inc.: 1-800-255-3924 (outside the U.S. 1-813-248-0585) POISON CONTROL CENTER: 800-222-1222 2. HAZARDS IDENTIFICATION Classification OSHA Regulatory Status This chemical is considered hazardous by the 2012 OSHA Hazard Communication Standard (29 CFR 1910.1200) Acute toxicity - Oral Category 4 Acute toxicity - Inhalation (Dusts/Mists) Category 4 Serious eye damage/eye irritation Category 1 Skin sensitization Category 1 Carcinogenicity Category 1A Reproductive toxicity Category 2 Label elements Emergency Overview Danger Hazard statements Harmful if swallowed Harmful if inhaled Causes serious eye damage May cause an allergic skin reaction May cause cancer Suspected of damaging fertility or the unborn child _____________________________________________________________________________________________
    [Show full text]
  • Antibiotic Resistance in Plant-Pathogenic Bacteria
    PY56CH08-Sundin ARI 23 May 2018 12:16 Annual Review of Phytopathology Antibiotic Resistance in Plant-Pathogenic Bacteria George W. Sundin1 and Nian Wang2 1Department of Plant, Soil, and Microbial Sciences, Michigan State University, East Lansing, Michigan 48824, USA; email: [email protected] 2Citrus Research and Education Center, Department of Microbiology and Cell Science, Institute of Food and Agricultural Sciences, University of Florida, Lake Alfred, Florida 33850, USA Annu. Rev. Phytopathol. 2018. 56:8.1–8.20 Keywords The Annual Review of Phytopathology is online at kasugamycin, oxytetracycline, streptomycin, resistome phyto.annualreviews.org https://doi.org/10.1146/annurev-phyto-080417- Abstract 045946 Antibiotics have been used for the management of relatively few bacterial Copyright c 2018 by Annual Reviews. plant diseases and are largely restricted to high-value fruit crops because of Access provided by INSEAD on 06/01/18. For personal use only. All rights reserved the expense involved. Antibiotic resistance in plant-pathogenic bacteria has Annu. Rev. Phytopathol. 2018.56. Downloaded from www.annualreviews.org become a problem in pathosystems where these antibiotics have been used for many years. Where the genetic basis for resistance has been examined, antibiotic resistance in plant pathogens has most often evolved through the acquisition of a resistance determinant via horizontal gene transfer. For ex- ample, the strAB streptomycin-resistance genes occur in Erwinia amylovora, Pseudomonas syringae,andXanthomonas campestris, and these genes have pre- sumably been acquired from nonpathogenic epiphytic bacteria colocated on plant hosts under antibiotic selection. We currently lack knowledge of the effect of the microbiome of commensal organisms on the potential of plant pathogens to evolve antibiotic resistance.
    [Show full text]
  • Socioeconomic Factors Associated with Antimicrobial Resistance Of
    01 Pan American Journal Original research of Public Health 02 03 04 05 06 Socioeconomic factors associated with antimicrobial 07 08 resistance of Pseudomonas aeruginosa, 09 10 Staphylococcus aureus, and Escherichia coli in Chilean 11 12 hospitals (2008–2017) 13 14 15 Kasim Allel,1 Patricia García,2 Jaime Labarca,3 José M. Munita,4 Magdalena Rendic,5 Grupo 16 6 5 17 Colaborativo de Resistencia Bacteriana, and Eduardo A. Undurraga 18 19 20 21 Suggested citation Allel K, García P, Labarca J, Munita JM, Rendic M; Grupo Colaborativo de Resistencia Bacteriana; et al. Socioeconomic fac- 22 tors associated with antimicrobial resistance of Pseudomonas aeruginosa, Staphylococcus aureus, and Escherichia coli in 23 Chilean hospitals (2008–2017). Rev Panam Salud Publica. 2020;44:e30. https://doi.org/10.26633/RPSP.2020.30 24 25 26 27 ABSTRACT Objective. To identify socioeconomic factors associated with antimicrobial resistance of Pseudomonas aeru- 28 ginosa, Staphylococcus aureus, and Escherichia coli in Chilean hospitals (2008–2017). 29 Methods. We reviewed the scientific literature on socioeconomic factors associated with the emergence and 30 dissemination of antimicrobial resistance. Using multivariate regression, we tested findings from the literature drawing from a longitudinal dataset on antimicrobial resistance from 41 major private and public hospitals and 31 a nationally representative household survey in Chile (2008–2017). We estimated resistance rates for three pri- 32 ority antibiotic–bacterium pairs, as defined by the Organisation for Economic Co-operation and Development; 33 i.e., imipenem and meropenem resistant P. aeruginosa, cloxacillin resistant S. aureus, and cefotaxime and 34 ciprofloxacin resistant E. coli. 35 Results.
    [Show full text]
  • The Use of Bactericides in Plant Agriculture with Reference to Use in Ci
    The Use of Bactericides in Plant Agriculture with Reference to Use in Ci... http://citrusrdf.org/use_of_bactericides_in_plant_ag_2016-02-04#more-4047 … Stephanie L. Slinski, Ph.D., Bactericide Project Manager, CRDF February 2016 The purpose of this communication is to discuss the use of bactericides in plant agriculture to control disease epidemics and the approaches that have been tested to control Huanglongbing (HLB) in citrus trees. The Citrus Research and Development Foundation (CRDF) has made this topic a priority in responding to HLB in Florida citrus. HLB is a disease devastating the citrus industry in Florida and throughout the world. Presently, no chemical treatment or resistant plant is available that will control the disease. For the Florida citrus industry to survive this epidemic, a chemical control will be necessary to suppress the disease, keeping the trees in production until groves can be replanted with resistant or tolerant varieties. This is similar to approaches taken during plant disease epidemics in other crops, which were eventually controlled by the planting of resistant varieties. Oxytetracycline, streptomycin sulfate and copper have been the main chemicals available to treat bacterial plant diseases in the US. The use of copper is limited to foliar diseases in regions where copper resistance is not widespread. Streptomycin and oxytetracycline are routinely used on some crops when copper is inadequate. Oxytetracycline has also often been used in the past to help manage plant disease epidemics. Research using bactericides on citrus suggests that chemical control may improve citrus tree health and contribute to sustaining the citrus industry in the current epidemic. Introduction The disease HLB has been known in many regions of the world for over a century.
    [Show full text]
  • Evaluation of Several Bactericides As Seed Treatments for the Control of Black Rot of Crucifers and Studies on an Antibacterial Substance from Cauliflower Seed
    Louisiana State University LSU Digital Commons LSU Historical Dissertations and Theses Graduate School 1962 Evaluation of Several Bactericides as Seed Treatments for the Control of Black Rot of Crucifers and Studies on an Antibacterial Substance From Cauliflower Seed. (Parts I and II). Fereydoon Malekzadeh Louisiana State University and Agricultural & Mechanical College Follow this and additional works at: https://digitalcommons.lsu.edu/gradschool_disstheses Recommended Citation Malekzadeh, Fereydoon, "Evaluation of Several Bactericides as Seed Treatments for the Control of Black Rot of Crucifers and Studies on an Antibacterial Substance From Cauliflower Seed. (Parts I and II)." (1962). LSU Historical Dissertations and Theses. 787. https://digitalcommons.lsu.edu/gradschool_disstheses/787 This Dissertation is brought to you for free and open access by the Graduate School at LSU Digital Commons. It has been accepted for inclusion in LSU Historical Dissertations and Theses by an authorized administrator of LSU Digital Commons. For more information, please contact [email protected]. This dissertation has been 63—2781 microfilmed exactly as received MALEKZADEH, Fereydoon, 1933- EVALUATION OF SEVERAL BACTERICIDES AS SEED TREATMENTS FOR THE CONTROL OF BLACK ROT OF CRUCIFERS AND STUDIES ON AN ANTIBACTERIAL SUBSTANCE FROM CAULI­ FLOWER SEED. (PARTS I AND II). Louisiana State University, Ph.D.,1962 Agriculture, plant pathology University Microfilms, Inc., Ann Arbor, Michigan EVALUATION OF SEVERAL BACTERICIDES AS SEED TREATMENTS FOR THE CONTROL OF BLACK ROT OF CRUCIFERS AND STUDIES ON AN ANTIBACTERIAL SUBSTANCE FROM CAULIFLOWER SEED A Dissertation Submitted to the Graduate Faculty of the Louisiana State University and Agricultural and Mechanical College in partial fulfillment of the requirements for the degree of Doctor of Philosophy in The Department of Botany and Plant Pathology by Fereydoon Malekzadeh B.Sc., University of Teheran, 1956 M .Sc., University of Teheran, 1958 August, 1962 ACKNOWLEDGMENT The writer wishes to express his sincere appreciation and gratitude to Dr.
    [Show full text]
  • Resistance to Cancer Chemotherapy
    Alfarouk et al. Cancer Cell Int (2015) 15:71 DOI 10.1186/s12935-015-0221-1 REVIEW Open Access Resistance to cancer chemotherapy: failure in drug response from ADME to P‑gp Khalid O Alfarouk1*, Christian‑Martin Stock2, Sophie Taylor3, Megan Walsh3, Abdel Khalig Muddathir4, Daniel Verduzco5, Adil H H Bashir1, Osama Y Mohammed6, Gamal O Elhassan7,8, Salvador Harguindey9, Stephan J Reshkin10, Muntaser E Ibrahim1 and Cyril Rauch3 Abstract Cancer chemotherapy resistance (MDR) is the innate and/or acquired ability of cancer cells to evade the effects of chemotherapeutics and is one of the most pressing major dilemmas in cancer therapy. Chemotherapy resistance can arise due to several host or tumor-related factors. However, most current research is focused on tumor-specific factors and specifically genes that handle expression of pumps that efflux accumulated drugs inside malignantly transformed types of cells. In this work, we suggest a wider and alternative perspective that sets the stage for a future platform in modifying drug resistance with respect to the treatment of cancer. Keywords: Drug, Resistance, Pharmacokinetics, ADME, pH, MDR Background Macroscopic (systemic) resistance [host–related In US only, the newly diagnosed cancer patient is factors] 1,665,540 every year and the estimated death is 585,720 One of the major effects of host-related factors that [1] which are increasing as countries become more devel- determine the activity of the drug is pharmacokinetic. oped and more people reach advanced ages. Therefore, Pharmacokinetics is defined as the action of the body in many efforts are being done in the war against cancer [2].
    [Show full text]
  • 1.11 Antidepressants and the Gut Microbiota
    UCC Library and UCC researchers have made this item openly available. Please let us know how this has helped you. Thanks! Title Effects of psychotropic drugs on the microbiota-gut-liver-brain axis Author(s) Cussotto, Sofia Publication date 2019 Original citation Cussotto, S. 2019. Effects of psychotropic drugs on the microbiota-gut- liver-brain axis. PhD Thesis, University College Cork. Type of publication Doctoral thesis Rights © 2019, Sofia Cussotto. http://creativecommons.org/licenses/by-nc-nd/3.0/ Item downloaded http://hdl.handle.net/10468/9468 from Downloaded on 2021-09-23T15:30:09Z Ollscoil na hÉireann, Corcaigh National University of Ireland, Cork Department of Anatomy and Neuroscience Head of Dept. John F. Cryan Effects of Psychotropic Drugs on the Microbiota-Gut-Liver-Brain Axis Thesis presented by Sofia Cussotto, MPharm Under the supervision of Prof. John F. Cryan Prof. Timothy G. Dinan For the degree of Doctor of Philosophy June 2019 Table of Contents Declaration ......................................................................................................... IV Author Contributions .......................................................................................... IV Acknowledgments ............................................................................................... V Publications and presentations ........................................................................... VI Abstract ............................................................................................................ VIII
    [Show full text]
  • Pharmacokinetic Drug Interactions of Antimicrobial Drugs: a Systematic Review on Oxazolidinones, Rifamycines, Macrolides, Fluoroquinolones, and Beta-Lactams
    Pharmaceutics 2011, 3, 865-913; doi:10.3390/pharmaceutics3040865 OPEN ACCESS Pharmaceutics ISSN 1999-4923 www.mdpi.com/journal/pharmaceutics Review Pharmacokinetic Drug Interactions of Antimicrobial Drugs: A Systematic Review on Oxazolidinones, Rifamycines, Macrolides, Fluoroquinolones, and Beta-Lactams Mathieu S. Bolhuis *, Prashant N. Panday, Arianna D. Pranger, Jos G. W. Kosterink and Jan-Willem C. Alffenaar Department of Hospital and Clinical Pharmacy, University Medical Center Groningen, University of Groningen, PO Box 30.001, 9700 RB Groningen, The Netherlands; E-Mails: [email protected] (P.N.P.); [email protected] (A.D.P.); [email protected] (J.G.W.K.); [email protected] (J.-W.C.A.) * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel.: +31-50-361-4071; Fax: +31-50-361-4078 Received: 15 October 2011; in revised form: 26 October 2011 / Accepted: 9 November 2011 / Published: 18 November 2011 Abstract: Like any other drug, antimicrobial drugs are prone to pharmacokinetic drug interactions. These drug interactions are a major concern in clinical practice as they may have an effect on efficacy and toxicity. This article provides an overview of all published pharmacokinetic studies on drug interactions of the commonly prescribed antimicrobial drugs oxazolidinones, rifamycines, macrolides, fluoroquinolones, and beta-lactams, focusing on systematic research. We describe drug-food and drug-drug interaction studies in humans, affecting antimicrobial drugs as well as concomitantly administered drugs. Since knowledge about mechanisms is of paramount importance for adequate management of drug interactions, the most plausible underlying mechanism of the drug interaction is provided when available.
    [Show full text]
  • Antibiotic Resistance: Mechanisms and New Antimicrobial Approaches
    Antibiotic Resistance This page intentionally left blank Antibiotic Resistance Mechanisms and New Antimicrobial Approaches Kateryna Kon, MD, PhD Department of Microbiology, Virology, and Immunology Kharkiv National Medical University Kharkiv, Ukraine Mahendra Rai, PhD Biotechnology Department SGB Amravati University Maharashtra, India AMSTERDAM • BOSTON • HEIDELBERG • LONDON NEW YORK • OXFORD • PARIS • SAN DIEGO SAN FRANCISCO • SINGAPORE • SYDNEY • TOKYO Academic Press is an imprint of Elsevier Academic Press is an imprint of Elsevier 125 London Wall, London EC2Y 5AS, UK 525 B Street, Suite 1800, San Diego, CA 92101-4495, USA 50 Hampshire Street, 5th Floor, Cambridge, MA 02139, USA The Boulevard, Langford Lane, Kidlington, Oxford OX5 1GB, UK Copyright r 2016 Elsevier Inc. All rights reserved. No part of this publication may be reproduced or transmitted in any form or by any means, electronic or mechanical, including photocopying, recording, or any information storage and retrieval system, without permission in writing from the publisher. Details on how to seek permission, further information about the Publisher’s permissions policies and our arrangements with organizations such as the Copyright Clearance Center and the Copyright Licensing Agency, can be found at our website: www.elsevier.com/permissions. This book and the individual contributions contained in it are protected under copyright by the Publisher (other than as may be noted herein). Notices Knowledge and best practice in this field are constantly changing. As new research and experience broaden our understanding, changes in research methods, professional practices, or medical treatment may become necessary. Practitioners and researchers must always rely on their own experience and knowledge in evaluating and using any information, methods, compounds, or experiments described herein.
    [Show full text]
  • Champion Fungicide/Bactericide EPA Reg
    MATERIAL SAFETY DATA SHEET ChampION++ Fungicide/Bactericide 1. CHEMICAL PRODUCT AND COMPANY IDENTIFICATION ++ Product Name: ChampION Fungicide/Bactericide EPA Reg. No.: 55146‐115 Synonyms: Copper Hydroxide, Copper Hydrate, Cupric Hydroxide Product Type: Fungicide / Bactericide Company Name: Nufarm Americas Inc., AGT Division 11901 S. Austin Avenue Alsip, IL 60803 Telephone Numbers: For Chemical Emergency, Spill, Leak, Fire, Exposure, or Accident, Call CHEMTREC Day or Night: 1‐800‐424‐9300 For Medical Emergencies Only, Call 1‐877‐325‐1840 Date of Issue: January 20, 2014 Supersedes: November 15, 2013 Sections Revised: Format, 4, 7 2. HAZARDS IDENTIFICATION Emergency Overview: Appearance and Odor: Blue‐green granular solid with a mild odor Warning Statements: Keep out of reach of children. CAUTION. Harmful if inhaled. Harmful if swallowed. Causes moderate eye irritation. Avoid contact with eyes or clothing. Avoid breathing dust. Potential Health Effects: Likely Routes of Exposure: Inhalation, eye and skin contact. Eye Contact: Mildly irritating based on toxicity studies. May cause tearing, pain, or blurred vision. Skin Contact: No more than slightly toxic and no more than slightly irritating by dermal exposure. Excessive exposure, especially if prolonged, may cause skin irritation. Repeated exposure may cause allergic contact dermatitis. Ingestion: Slightly toxic by oral exposure. This material may produce toxicity if ingested in large quantities. Symptoms of overexposure may include nausea and vomiting, abdominal pain, and central nervous system depression, which, if severe enough, may lead to death. Inhalation: Slightly toxic by inhalation. Overexposure by inhalation may cause cough, mucous production, shortness of breath, reflecting metal fume fever. Medical Conditions Aggravated by Exposure: Copper intolerant individuals should not be exposed to this material.
    [Show full text]
  • SAFETY DATA SHEET Junction® Fungicide/Bactericide
    SDS Junction Fungicide/Bactericide Conforms to HazCom 2012/United States SAFETY DATA SHEET Junction® Fungicide/Bactericide Section 1. Identification ® GHS product identifier: Junction Fungicide/Bactericide Recommended use of the chemical and restrictions on use Identified uses: Fungicide/Bactericide EPA Registration No.: 67690-35 Supplier's details: SePRO Corporation 11550 North Meridian Street Suite 600 Carmel, IN 46032 U.S.A. Tel: 317-580-8282/Toll free: 1-800-419-7779 Fax: 317-580-8290 Monday - Friday, 8am to 5pm E.S.T. www.sepro.com Emergency telephone number: INFOTRAC – 24-hour service 1-800-535-5053 The following recommendations for exposure controls and personal protection are intended for the manufacture, formulation and packaging of this product. For applications and/or use, consult the product label. The label directions supersede the text of this Safety Data Sheet for application and/or use. Section 2. Hazards identification OSHA/HCS status: This material is considered hazardous by the OSHA Hazard Communication Standard (29 CFR 1910.1200). Classification of the substance or mixture: ACUTE TOXICITY – ORAL - Category 4 ACUTE TOXICITY – INHALATION (DUST/MISTS) – Category 4 SERIOUS EYE DAMAGE/EYE IRRITATION – Category 1 SKIN SENSITIZATION – Category 1 CARCINOGENICITY – Category 1A REPRODUCTIVE TOXICITY – Category 2 GHS label elements Hazard pictograms: Signal word: Danger Page 1 of 12 SDS Junction Fungicide/Bactericide Hazard statements: Harmful if swallowed Harmful if inhaled Causes serious eye damage May cause an allergic skin
    [Show full text]