Seminar on Drug Chirality
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Schistosoma Mansoni
Pharmacological and pharmacokinetic studies on trematocidal drugs : praziquantel and two synthetic peroxide lead candidates INAUGURALDISSERTATION zur Erlangung der Würde eines Doktors der Philosophie vorgelegt der Philosophisch-Naturwissenschaftlichen Fakultät der Universität Basel von Isabel Meister aus Neuchâtel (NE) Basel, 2017 Originaldokument gespeichert auf dem Dokumentenserver der Universität Basel edoc.unibas.ch This work is licensed under a Creative Commons Attribution 4.0 International License. Genehmigt von der Philosophisch-Naturwissenschaftlichen Fakultät auf Antrag von Prof. Dr. Jennifer Keiser Prof. Dr. Piero Olliaro Basel, den 23. Juni 2015 Prof. Dr. Jörg Schibler Dekan Table of Contents Acknowledgements ................................................................................................................................ III Summary ................................................................................................................................................. V List of abbreviations ............................................................................................................................ VII Chapter 1. General introduction ..............................................................................................1 1.1 Trematode biology and life cycle ...............................................................................................2 1.2 Epidemiology and clinical aspects .............................................................................................5 -
Consensus for the Management of Analgesia, Sedation and Delirium in Adults with COVID-19-Associated Acute Respiratory Distress Syndrome
ARTIGO ESPECIAL Manuel Donato1,2,3 , Federico Carlos Carini4 , María Julia Meschini5, Ignacio López Saubidet6 , Consenso para el manejo de la analgesia, sedación Adela Goldberg7, Marisol García Sarubio5, Daniela Olmos8, Rosa Reina5 em nombre del Comité de y delirium en adultos con síndrome de distrés Analgesia, Sedación y Delirium de la Sociedad Argentina de Terapia Intensiva respiratorio agudo por COVID-19 Consensus for the management of analgesia, sedation and delirium in adults with COVID-19-associated acute respiratory distress syndrome 1. Hospital General de Agudos José María Penna RESUMEN Sedación y Delirium de la Sociedad - Buenos Aires, Argentina. Argentina de Terapia Intensiva. 2. Ministerio de Salud de la Nación Argentina – Objetivo: Proponer estrategias Resultados: Se acordaron Buenos Aires, Argentina. agile para este abordaje integral de 3. Instituto de Efectividad Clínica y Sanitaria - recomendaciones y se desarrollaron la analgesia, sedación, delirium, Buenos Aires, Argentina. herramientas para asegurar un 4. Hospital Italiano de Buenos Aires - Buenos implementación de movilidad abordaje integral de analgesia, Aires, Argentina. temprana e inclusión familiar del sedación, delirium, implementación 5. Hospital Interzonal General de Agudos General paciente con síndrome de dificultad San Martín - La Plata, Argentina. de movilidad temprana e inclusión respiratoria aguda por COVID-19, 6. Centro de Educación Médica e Investigaciones familiar del paciente adulto con Clínicas “Norberto Quirno” - Buenos Aires, Argentina. considerando el alto riesgo de infección síndrome de dificultad respiratoria 7. Sanatorio de La Trinidad Mitre - Buenos Aires, que existe entre los trabajadores de Argentina. aguda por COVID-19. salud, el tratamiento humanitario 8. Hospital Municipal Príncipe de Asturias - Córdoba, Discusión: Ante el nuevo orden Argentina. -
Chiral Drugs for You and Me
Teaching Chemistry Through The Jigsaw Strategy Example 1 Topic Thalidomide: A Controversial Chiral Drug Subtopics 1. Why is drug chirality important? 2. What caused the thalidomide tragedy? 3. Why has thalidomide been approved for sale again? Level Secondary 6-7 Curriculum Links Stereoisomerism Enantiomerism Chiral carbon compounds Medium of instruction English Copyright © 2007 by Quality Education Fund, Hong Kong All rights reserved. Prepared by Professor Derek Cheung, The Department of Curriculum and Instruction, The Chinese University of Hong Kong. No part of this document may be reproduced in any manner whatsoever without written permission, except in the case of use as instructional material in a school by a teacher. 1 1. Why is drug chirality important? Enantiomers are optical isomers which are nonsuperimposable mirror-image structures. The property of nonsuperimposability is called chirality. A molecule is chiral if and only if it is not superimposable on its mirror image. The most common chiral centre is carbon. When four nonidentical atoms or groups are attached to a tetravalent carbon, the tetrahedral arrangement of the bonds in space results in two enantiomers. Enantiomers can be distinguished by experiments because they have different ability to rotate a beam of plane-polarized light: to the clockwise direction as a dextrorotatory (+)-enantiomer and to the counterclockwise direction as a levorotatory (-)-enantiomer. A mixture of equal portions (50/50) of the (+) and (-) enantiomers is called a racemic mixture. In 1957, a pharmaceutical company in West Germany introduced a new drug to the market. It was called thalidomide with molecular formula C13H10N2O4. The drug was sold in 46 countries under at least 37 brand names. -
Test Summary Sheet For
Test Summary Sheet for: 8054B Postmortem, Expanded with NPS, Blood (Forensic) The following test codes are contained in this document: 1. 8054B Postmortem, Expanded with NPS, Blood (Forensic) 2. 50000B Acetaminophen Confirmation, Blood (Forensic) 3. 52250B Alcohols and Acetone Confirmation, Blood (Forensic) 4. 52143B Alfentanil and Sufentanil Confirmation, Blood (Forensic) 5. 52168B Amitriptyline and Metabolite Confirmation, Blood (Forensic) 6. 52239B Amoxapine Confirmation, Blood (Forensic) 7. 52485B Amphetamines Confirmation, Blood (Forensic) 8. 52416B Aripiprazole Confirmation, Blood (Forensic) 9. 52007B Atomoxetine Confirmation, Blood (Forensic) 10. 50011B Barbiturates Confirmation, Blood (Forensic) 11. 52365B Bath Salts Confirmation, Blood (Forensic) 12. 52367B Bath Salts Confirmation, Blood (Forensic) 13. 50012B Benzodiazepines Confirmation, Blood (Forensic) 14. 52443B Benztropine Confirmation, Blood (Forensic) 15. 52245B Brompheniramine Confirmation, Blood (Forensic) 16. 52011B Bupivacaine Confirmation, Blood (Forensic) 17. 52012B Bupropion and Metabolite Confirmation, Blood (Forensic) 18. 52444B Buspirone Confirmation, Blood (Forensic) 19. 52198B Cannabinoids Confirmation, Blood (Forensic) 20. 52015B Carbamazepine and Metabolite Confirmation, Blood (Forensic) 21. 52017B Carisoprodol and Metabolite Confirmation, Blood (Forensic) 22. 52440B Chlorpheniramine Confirmation, Blood (Forensic) 23. 52272B Chlorpromazine Confirmation, Blood (Forensic) 24. 52482B Citalopram Confirmation, Blood (Forensic) 25. 52274B Clomipramine and Metabolite -
Abstract CHIRALITY and ENANTIOMERS CHIRAL DRUGS in BIOLOGICAL SYSTEMS
Abstract CHIRALITY AND ENANTIOMERS This section contains the basics needed to understand chiral drugs. Undergraduate textbooks in chemistry are good resources for a more thorough discussion of chirality and enantiomers. The most important point is that chiral drugs have 2 structurally similar forms that can behave very differently in biological systems due to their different shapes in 3-dimensional space. These 2 possible forms are termed enantiomers, and the 2 enantiomers of a given chiral drug should be considered 2 different drugs. This topic is discussed further in the next section. Chirality is formally defined as the geometric property of a rigid object (like a molecule or drug) of not being superimposable with its mirror image. Molecules that can be superimposed on their mirror images are achiral (not chiral). Chirality is a property of matter found throughout biological systems, from the basic building blocks of life such as amino acids, carbohydrates, and lipids to the layout of the human body. Chirality is often illustrated with the idea of left- and right-handedness: a left hand and right hand are mirror images of each other but are not superimposable. The 2 mirror images of a chiral molecule are termed enantiomers. Like hands, enantiomers come in pairs. Both molecules of an enantiomer pair have the same chemical composition and can be drawn the same way in 2 dimensions (e.g., a drug structure on a package insert), but in chiral environments such as the receptors and enzymes in the body, they can behave differently. A racemate (often called a racemic mixture) is a mixture of equal amounts of both enantiomers of a chiral drug. -
Enantiomeric Quantification of Psychoactive Substances and Beta Blockers by Gas Chromatography-Mass Spectrometry in Influents of Wastewater Treatment Plants
Enantiomeric quantification of psychoactive substances and beta blockers by gas chromatography-mass spectrometry in influents of wastewater treatment plants Ricardo Daniel Teixeira Gonçalves Dissertation of the 2nd Cycle of Studies Conducive to the Master’s Degree in Clinical and Forensic Analytical Toxicology, Faculty of Pharmacy, University of Porto Work performed under the orientation of: Professor Doctor Maria Elizabeth Tiritan Professor Doctor Cláudia Maria Rosa Ribeiro September 2018 IT IS NOT PERMITED TO REPRODUCE ANY PART OF THIS DISSERTATION DE ACORDO COM A LEGISLAÇÃO EM VIGOR, NÃO É PERMITIDA A REPRODUÇÃO DE QUALQUER PARTE DESTA DISSERTAÇÃO Agradecimentos Em primeiro lugar gostaria de agradecer às minhas orientadoras (ou mães da ciência), a Professora Doutora Maria Elizabeth Tiritan e a Professora Doutora Cláudia Ribeiro por me terem aceitado (adotado) para poder continuar este projeto. Obrigado por me ajudarem na iniciação de um projeto de raiz, que depois de quatro anos e muitas frustrações, vejo que não foi em vão. Por toda a ajuda, insistência, paciência, preocupação e compreensão que sempre tiveram, o maior obrigado! À Dra. Sara Cravo do laboratório de química orgânica da FFUP, que me recebeu de braços abertos, batalhou comigo durante meses e me deixou usar e abusar do seu laboratório de cromatografia gasosa. Obrigado por toda a ajuda, paciência, explicações, disponibilidade e acima de tudo, por me compreender nos momentos mais desesperantes. Estou-lhe profundamente grato por me fazer sentir “em casa” e por sempre arranjar soluções! Ao Professor Doutor Carlos Afonso do laboratório de química orgânica da FFUP por me autorizar a invadir o laboratório de química orgânica e pela preocupação constante com o progresso do trabalho. -
(12) Patent Application Publication (10) Pub. No.: US 2005/0033522 A1 Wainer Et Al
US 20050033522A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0033522 A1 Wainer et al. (43) Pub. Date: Feb. 10, 2005 (54) COMPUTER-BASED MODEL FOR Related U.S. Application Data IDENTIFICATION AND CHARACTERIZATION OF (63) Continuation-in-part of application No. 10/411,206, NON-COMPETITIVE INHIBITORS OF filed on Apr. 11, 2003. NCOTINIC ACETYLCHOLINE RECEPTORS AND RELATED LIGAND-GATED ON Publication Classification CHANNEL RECEPTORS (51) Int. Cl." .......................... G06F 19/00; G01N 33/48; (76) Inventors: Irving W. Wainer, Washington, DC GO1N 33/50 (US); Krzysztof Jozwiak, Abingdon, (52) U.S. Cl. ................................................................ 702/19 MD (US); Ruin Moaddel, Germantown, MD (US); Sarangan (57) ABSTRACT Ravichandran, Frederick, MD (US); A computer readable medium holding data of a molecular Jack R. Collins, Frederick, MD (US) model of a ligand-gated ion channel receptor and/or a computer System for modeling Said receptor are provided by Correspondence Address: the instant invention. The molecular model can be used to BRCH STEWART KOLASCH & BRCH design novel compounds having activity as non-competitive PO BOX 747 inhibitors of the ion channel. A preferred embodiment of the FALLS CHURCH, VA 22040-0747 (US) invention relates to nicotinic acetylcholine receptorS. Com pounds having activity as non-competitive inhibitors of (21) Appl. No.: 10/820,809 ligand-gated ion channel receptors and methods for inhib iting the receptor and treating diseases or disorderS mediated (22) Filed: Apr. 9, 2004 by function of the receptor are also disclosed. Patent Application Publication Feb. 10, 2005 Sheet 1 of 16 US 2005/0033522 A1 ONE SUBUNT OF nAChR - N NH2 UGAND-BINDING STE Soffee CROSS-SECTION OF FME ASSEMBLED SUBUNITS (2xa + 3x p) OF nAChR i: T. -
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI
Dr. Duke's Phytochemical and Ethnobotanical Databases List of Chemicals for Chronic Venous Insufficiency/CVI Chemical Activity Count (+)-AROMOLINE 1 (+)-CATECHIN 5 (+)-GALLOCATECHIN 1 (+)-HERNANDEZINE 1 (+)-PRAERUPTORUM-A 1 (+)-SYRINGARESINOL 1 (+)-SYRINGARESINOL-DI-O-BETA-D-GLUCOSIDE 1 (-)-ACETOXYCOLLININ 1 (-)-APOGLAZIOVINE 1 (-)-BISPARTHENOLIDINE 1 (-)-BORNYL-CAFFEATE 1 (-)-BORNYL-FERULATE 1 (-)-BORNYL-P-COUMARATE 1 (-)-CANADINE 1 (-)-EPICATECHIN 4 (-)-EPICATECHIN-3-O-GALLATE 1 (-)-EPIGALLOCATECHIN 1 (-)-EPIGALLOCATECHIN-3-O-GALLATE 2 (-)-EPIGALLOCATECHIN-GALLATE 3 (-)-HYDROXYJASMONIC-ACID 1 (-)-N-(1'-DEOXY-1'-D-FRUCTOPYRANOSYL)-S-ALLYL-L-CYSTEINE-SULFOXIDE 1 (1'S)-1'-ACETOXYCHAVICOL-ACETATE 1 (2R)-(12Z,15Z)-2-HYDROXY-4-OXOHENEICOSA-12,15-DIEN-1-YL-ACETATE 1 (7R,10R)-CAROTA-1,4-DIENALDEHYDE 1 (E)-4-(3',4'-DIMETHOXYPHENYL)-BUT-3-EN-OL 1 1,2,6-TRI-O-GALLOYL-BETA-D-GLUCOSE 1 1,7-BIS(3,4-DIHYDROXYPHENYL)HEPTA-4E,6E-DIEN-3-ONE 1 Chemical Activity Count 1,7-BIS(4-HYDROXY-3-METHOXYPHENYL)-1,6-HEPTADIEN-3,5-DIONE 1 1,8-CINEOLE 1 1-(METHYLSULFINYL)-PROPYL-METHYL-DISULFIDE 1 1-ETHYL-BETA-CARBOLINE 1 1-O-(2,3,4-TRIHYDROXY-3-METHYL)-BUTYL-6-O-FERULOYL-BETA-D-GLUCOPYRANOSIDE 1 10-ACETOXY-8-HYDROXY-9-ISOBUTYLOXY-6-METHOXYTHYMOL 1 10-GINGEROL 1 12-(4'-METHOXYPHENYL)-DAURICINE 1 12-METHOXYDIHYDROCOSTULONIDE 1 13',II8-BIAPIGENIN 1 13-HYDROXYLUPANINE 1 14-ACETOXYCEDROL 1 14-O-ACETYL-ACOVENIDOSE-C 1 16-HYDROXY-4,4,10,13-TETRAMETHYL-17-(4-METHYL-PENTYL)-HEXADECAHYDRO- 1 CYCLOPENTA[A]PHENANTHREN-3-ONE 2,3,7-TRIHYDROXY-5-(3,4-DIHYDROXY-E-STYRYL)-6,7,8,9-TETRAHYDRO-5H- -
Analytical Separations Using Packed and Open-Tubular Capillary Electrochromatography" (2004)
Louisiana State University LSU Digital Commons LSU Doctoral Dissertations Graduate School 2004 Analytical separations using packed and open- tubular capillary electrochromatography Constantina P. Kapnissi Louisiana State University and Agricultural and Mechanical College, [email protected] Follow this and additional works at: https://digitalcommons.lsu.edu/gradschool_dissertations Part of the Chemistry Commons Recommended Citation Kapnissi, Constantina P., "Analytical separations using packed and open-tubular capillary electrochromatography" (2004). LSU Doctoral Dissertations. 595. https://digitalcommons.lsu.edu/gradschool_dissertations/595 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 Doctoral Dissertations by an authorized graduate school editor of LSU Digital Commons. For more information, please [email protected]. ANALYTICAL SEPARATIONS USING PACKED AND OPEN- TUBULAR CAPILLARY ELECTROCHROMATOGRAPHY 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 Chemistry by Constantina P. Kapnissi B.S., University of Cyprus, 1999 August 2004 Copyright 2004 Constantina Panayioti Kapnissi All rights reserved ii DEDICATION I would like to dedicate this work to my husband Andreas Christodoulou, my parents Panayiotis and Eleni Kapnissi, and my sisters Erasmia, Panayiota and Stella Kapnissi. I want to thank all of you for helping me, in your own way, to finally make one of my dreams come true. Thank you for encouraging me to continue and achieve my goals. Thank you for your endless love, support, and motivation. Andreas, thank you for your continuous patience and for being there for me whenever I needed you during this difficult time. -
First Chemoenzymatic Stereodivergent Synthesis of Both Enantiomers of Promethazine and Ethopropazine
First chemoenzymatic stereodivergent synthesis of both enantiomers of promethazine and ethopropazine Paweł Borowiecki*, Daniel Paprocki and Maciej Dranka Full Research Paper Open Access Address: Beilstein J. Org. Chem. 2014, 10, 3038–3055. Warsaw University of Technology, Faculty of Chemistry, doi:10.3762/bjoc.10.322 Noakowskiego St. 3, 00-664 Warsaw, Poland Received: 03 September 2014 Email: Accepted: 01 December 2014 Paweł Borowiecki* - [email protected] Published: 18 December 2014 * Corresponding author Associate Editor: J. Aubé Keywords: © 2014 Borowiecki et al; licensee Beilstein-Institut. ethopropazine; lipase-catalyzed kinetic resolution; Mosher License and terms: see end of document. methodology; promethazine; stereodivergent synthesis Abstract Enantioenriched promethazine and ethopropazine were synthesized through a simple and straightforward four-step chemoenzy- matic route. The central chiral building block, 1-(10H-phenothiazin-10-yl)propan-2-ol, was obtained via a lipase-mediated kinetic resolution protocol, which furnished both enantiomeric forms, with superb enantioselectivity (up to E = 844), from the racemate. Novozym 435 and Lipozyme TL IM have been found as ideal biocatalysts for preparation of highly enantioenriched phenothiazolic alcohols (up to >99% ee), which absolute configurations were assigned by Mosher’s methodology and unambiguously confirmed by XRD analysis. Thus obtained key-intermediates were further transformed into bromide derivatives by means of PBr3, and subse- quently reacted with appropriate amine providing desired pharmacologically valuable (R)- and (S)-stereoisomers of title drugs in an ee range of 84–98%, respectively. The modular amination procedure is based on a solvent-dependent stereodivergent transforma- tion of the bromo derivative, which conducted in toluene gives mainly the product of single inversion, whereas carried out in methanol it provides exclusively the product of net retention. -
Handbook of Drugs in Intensive Care: an A
This page intentionally left blank This page intentionally left blank Handbook of Drugs in Intensive Care Fourth edition This book is dedicated to Georgina Paw Handbook of Drugs in Intensive Care An A-Z Guide Fourth edition Henry G W Paw BPharm MRPharmS MBBS FRCA Consultant in Anaesthesia and Intensive Care York Hospital York Rob Shulman BSc (Pharm) MRPharmS Dip Clin Pham, DHC (Pharm) Lead Pharmacist in Critical Care University College London Hospitals London CAMBRIDGE UNIVERSITY PRESS Cambridge, New York, Melbourne, Madrid, Cape Town, Singapore, São Paulo, Delhi, Dubai, Tokyo Cambridge University Press The Edinburgh Building, Cambridge CB2 8RU, UK Published in the United States of America by Cambridge University Press, New York www.cambridge.org Information on this title: www.cambridge.org/9780521757157 © H. Paw and R. Shulman 2010 This publication is in copyright. Subject to statutory exception and to the provision of relevant collective licensing agreements, no reproduction of any part may take place without the written permission of Cambridge University Press. First published in print format 2010 ISBN-13 978-0-521-75715-7 Paperback Cambridge University Press has no responsibility for the persistence or accuracy of urls for external or third-party internet websites referred to in this publication, and does not guarantee that any content on such websites is, or will remain, accurate or appropriate. CONTENTS Introduction vii How to use this book viii Abbreviations x Acknowledgements xiii DRUGS: An A–Z Guide 1 SHORT NOTES 229 Routes of -
University of Lucknow Masters of Pharmaceutical Chemistry Programme Regulation 2020
UNIVERSITY OF LUCKNOW MASTERS OF PHARMACEUTICAL CHEMISTRY PROGRAMME REGULATION 2020 1. Applicability These regulations shall apply to the Masters in Pharmaceutical Chemistry programme from the session 2020-21. 2. Minimum eligibility for admission A three/four years Bachelor’s degree or equivalent with chemistry as one of the subject in final year awarded by University or Institute established as per law and recognized as equivalent by university with minimum 45% marks for general and OBC (SC/ST 40%) or equivalent grade shall constitute the minimum requirement for admission to the Masters in Pharmaceutical Chemistry Programme 3. Programme Objectives i. To enable the students to understand the basic concepts of bio-inorganic, bio- organic, physical chemistry, analytical chemistry, drug formulation, drug design and development. ii. To develop the ability to present pharmaceutical chemistry research by means of an oral presentation, a scientific poster or a written report. iii. To be able to use and apply professional softwares relevant to chemistry. iv. To equip the students with the knowledge to develop Pharmaceutically important molecules, new drug delivery systems etc. v. To learn the application of analytical tools for determination of organic molecules and to generate validation protocol for all pharmaceutical operations starting from drug research to development to formulation. vi. To learn the Mechanism of Action of various class of drugs. vii. To learn the brief overview of the use of various drugs in treatment of various diseases. 4. Programme Outcomes PO-1. Demonstrate, solve and an understanding of major concepts in all disciplines of Chemistry independently and in group as well as draw logical conclusions through Project and Seminar Presentation.