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Thesis of Potentially Sweet Dihydrochalcone Glycosides
University of Bath PHD The synthesis of potentially sweet dihydrochalcone glycosides. Noble, Christopher Michael Award date: 1974 Awarding institution: University of Bath Link to publication Alternative formats If you require this document in an alternative format, please contact: [email protected] General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. • Users may download and print one copy of any publication from the public portal for the purpose of private study or research. • You may not further distribute the material or use it for any profit-making activity or commercial gain • You may freely distribute the URL identifying the publication in the public portal ? Take down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. Download date: 05. Oct. 2021 THE SYNTHESIS OF POTBTTIALLY SWEET DIHYDROCHALCOITB GLYCOSIDES submitted by CHRISTOPHER MICHAEL NOBLE for the degree of Doctor of Philosophy of the University of Bath. 1974 COPYRIGHT Attention is drawn to the fact that copyright of this thesis rests with its author.This copy of the the sis has been supplied on condition that anyone who con sults it is understood to recognise that its copyright rests with its author and that no quotation from the thesis and no information derived from it may be pub lished without the prior written consent of the author. -
Picrotoxin-Like Channel Blockers of GABAA Receptors
COMMENTARY Picrotoxin-like channel blockers of GABAA receptors Richard W. Olsen* Department of Molecular and Medical Pharmacology, Geffen School of Medicine, University of California, Los Angeles, CA 90095-1735 icrotoxin (PTX) is the prototypic vous system. Instead of an acetylcholine antagonist of GABAA receptors (ACh) target, the cage convulsants are (GABARs), the primary media- noncompetitive GABAR antagonists act- tors of inhibitory neurotransmis- ing at the PTX site: they inhibit GABAR Psion (rapid and tonic) in the nervous currents and synapses in mammalian neu- system. Picrotoxinin (Fig. 1A), the active rons and inhibit [3H]dihydropicrotoxinin ingredient in this plant convulsant, struc- binding to GABAR sites in brain mem- turally does not resemble GABA, a sim- branes (7, 9). A potent example, t-butyl ple, small amino acid, but it is a polycylic bicyclophosphorothionate, is a major re- compound with no nitrogen atom. The search tool used to assay GABARs by compound somehow prevents ion flow radio-ligand binding (10). through the chloride channel activated by This drug target appears to be the site GABA in the GABAR, a member of the of action of the experimental convulsant cys-loop, ligand-gated ion channel super- pentylenetetrazol (1, 4) and numerous family. Unlike the competitive GABAR polychlorinated hydrocarbon insecticides, antagonist bicuculline, PTX is clearly a including dieldrin, lindane, and fipronil, noncompetitive antagonist (NCA), acting compounds that have been applied in not at the GABA recognition site but per- huge amounts to the environment with haps within the ion channel. Thus PTX major agricultural economic impact (2). ͞ appears to be an excellent example of al- Some of the other potent toxicants insec- losteric modulation, which is extremely ticides were also radiolabeled and used to important in protein function in general characterize receptor action, allowing and especially for GABAR (1). -
Qrno. 1 2 3 4 5 6 7 1 CP 2903 77 100 0 Cfcl3
QRNo. General description of Type of Tariff line code(s) affected, based on Detailed Product Description WTO Justification (e.g. National legal basis and entry into Administration, modification of previously the restriction restriction HS(2012) Article XX(g) of the GATT, etc.) force (i.e. Law, regulation or notified measures, and other comments (Symbol in and Grounds for Restriction, administrative decision) Annex 2 of e.g., Other International the Decision) Commitments (e.g. Montreal Protocol, CITES, etc) 12 3 4 5 6 7 1 Prohibition to CP 2903 77 100 0 CFCl3 (CFC-11) Trichlorofluoromethane Article XX(h) GATT Board of Eurasian Economic Import/export of these ozone destroying import/export ozone CP-X Commission substances from/to the customs territory of the destroying substances 2903 77 200 0 CF2Cl2 (CFC-12) Dichlorodifluoromethane Article 46 of the EAEU Treaty DECISION on August 16, 2012 N Eurasian Economic Union is permitted only in (excluding goods in dated 29 may 2014 and paragraphs 134 the following cases: transit) (all EAEU 2903 77 300 0 C2F3Cl3 (CFC-113) 1,1,2- 4 and 37 of the Protocol on non- On legal acts in the field of non- _to be used solely as a raw material for the countries) Trichlorotrifluoroethane tariff regulation measures against tariff regulation (as last amended at 2 production of other chemicals; third countries Annex No. 7 to the June 2016) EAEU of 29 May 2014 Annex 1 to the Decision N 134 dated 16 August 2012 Unit list of goods subject to prohibitions or restrictions on import or export by countries- members of the -
Studies on the Pharmacology of Conopharyngine, an Indole Alkaloid of the Voacanga Series
Br. J. Pharmac. Chemother. (1967), 30, 173-185. STUDIES ON THE PHARMACOLOGY OF CONOPHARYNGINE, AN INDOLE ALKALOID OF THE VOACANGA SERIES BY P. R. CARROLL AND G. A. STARMER From the Department of Pharmacology, University of Sydney, New South Wales, Australia (Received January 17, 1967) Conopharyngine, the major alkaloid present in the leaves of Tabernaemontana (Conopharyngia) pachysiphon var. cumminsi (Stapf) H. Huber was isolated and identified by Thomas & Starmer (1963). The same alkaloid has also been found in the stem bark of a Nigerian variety of the same species by Patel & Poisson (1966) and in the stem bark of Conopharyngia durissima by Renner, Prins & Stoll (1959). Conopharyn- gine is an indole alkaloid of the voacanga type, being 18-carbomethoxy-12,13- dimethoxyibogamine (Fig. 1) and is thus closely related to voacangine and coronaridine. Me.0OC Fig. 1. Conopharyngine (18-carbomethoxy-12,13-dimethoxyibogamine). Some confusion exists in that an alkaloid with an entirely different structure, but also named conopharyngine, was isolated from a cultivated variety of Conopharyngia pachysiphon by Dickel, Lucas & Macphillamy (1959). This compound was shown to be the 3-D-9-glucoside of 55-20a-amino-3 8-hydroxypregnene, and was reported to possess marked hypotensive properties. The presence of steroid alkaloids in the Tabernaemontaneae was hitherto unknown and it was suggested by Raffauf & Flagler (1960) and Bisset (1961) that the plant material was open to further botanical confir- mation. The roots of the conopharyngia species are used in West Africa to treat fever (Kennedy, 1936), including that of malaria (Watt & Breyer-Brandwijk, 1962). The only report on the pharmacology of conopharyngine is that of Zetler (1964), who included it in a study of some of the effects of 23 natural and semi-synthetic alkaloids 174 P. -
AHFS Pharmacologic-Therapeutic Classification System
AHFS Pharmacologic-Therapeutic Classification System Abacavir 48:24 - Mucolytic Agents - 382638 8:18.08.20 - HIV Nucleoside and Nucleotide Reverse Acitretin 84:92 - Skin and Mucous Membrane Agents, Abaloparatide 68:24.08 - Parathyroid Agents - 317036 Aclidinium Abatacept 12:08.08 - Antimuscarinics/Antispasmodics - 313022 92:36 - Disease-modifying Antirheumatic Drugs - Acrivastine 92:20 - Immunomodulatory Agents - 306003 4:08 - Second Generation Antihistamines - 394040 Abciximab 48:04.08 - Second Generation Antihistamines - 394040 20:12.18 - Platelet-aggregation Inhibitors - 395014 Acyclovir Abemaciclib 8:18.32 - Nucleosides and Nucleotides - 381045 10:00 - Antineoplastic Agents - 317058 84:04.06 - Antivirals - 381036 Abiraterone Adalimumab; -adaz 10:00 - Antineoplastic Agents - 311027 92:36 - Disease-modifying Antirheumatic Drugs - AbobotulinumtoxinA 56:92 - GI Drugs, Miscellaneous - 302046 92:20 - Immunomodulatory Agents - 302046 92:92 - Other Miscellaneous Therapeutic Agents - 12:20.92 - Skeletal Muscle Relaxants, Miscellaneous - Adapalene 84:92 - Skin and Mucous Membrane Agents, Acalabrutinib 10:00 - Antineoplastic Agents - 317059 Adefovir Acamprosate 8:18.32 - Nucleosides and Nucleotides - 302036 28:92 - Central Nervous System Agents, Adenosine 24:04.04.24 - Class IV Antiarrhythmics - 304010 Acarbose Adenovirus Vaccine Live Oral 68:20.02 - alpha-Glucosidase Inhibitors - 396015 80:12 - Vaccines - 315016 Acebutolol Ado-Trastuzumab 24:24 - beta-Adrenergic Blocking Agents - 387003 10:00 - Antineoplastic Agents - 313041 12:16.08.08 - Selective -
Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany). -
Fluorides in the Environment
Color profile: Disabled Composite 150 lpi at 45 degrees Fluorides in the Environment A4662 - Weinstein - Vouchers - VP10 #K.prn 1 Z:\Customer\CABI\A4642 - Weinstein\A4662 - Weinstein - Vouchers - VP10 #K.vp Monday, November 10, 2003 3:35:50 PM Color profile: Disabled Composite 150 lpi at 45 degrees A4662 - Weinstein - Vouchers - VP10 #K.prn 2 Z:\Customer\CABI\A4642 - Weinstein\A4662 - Weinstein - Vouchers - VP10 #K.vp Monday, November 10, 2003 3:35:50 PM Color profile: Disabled Composite 150 lpi at 45 degrees Fluorides in the Environment Effects on Plants and Animals Professor L.H. Weinstein Boyce Thompson Institute for Plant Research Tower Road Ithaca NY 14853 USA and Professor A. Davison School of Biology Ridley Building University of Newcastle Newcastle upon Tyne NE1 7RU UK CABI Publishing A4662 - Weinstein - Vouchers - VP10 #K.prn 3 Z:\Customer\CABI\A4642 - Weinstein\A4662 - Weinstein - Vouchers - VP10 #K.vp Monday, November 10, 2003 3:35:51 PM Color profile: Disabled Composite 150 lpi at 45 degrees CABI Publishing is a division of CAB International CABI Publishing CABI Publishing CAB International 875 Massachusetts Avenue Wallingford 7th Floor Oxon OX10 8DE Cambridge, MA 02139 UK USA Tel: +44 (0)1491 832111 Tel: +1 617 395 4056 Fax: +44 (0)1491 833508 Fax: +1 617 354 6875 E-mail: [email protected] E-mail: [email protected] Web site: www.cabi-publishing.org ©L.H. Weinstein and A. Davison 2004. All rights reserved. No part of this publication may be reproduced in any form or by any means, electronically, mechanically, by photocopying, recording or otherwise, without the prior permission of the copyright owners. -
1-(4-Amino-Cyclohexyl)
(19) & (11) EP 1 598 339 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 211/04 (2006.01) C07D 211/06 (2006.01) 24.06.2009 Bulletin 2009/26 C07D 235/24 (2006.01) C07D 413/04 (2006.01) C07D 235/26 (2006.01) C07D 401/04 (2006.01) (2006.01) (2006.01) (21) Application number: 05014116.7 C07D 401/06 C07D 403/04 C07D 403/06 (2006.01) A61K 31/44 (2006.01) A61K 31/48 (2006.01) A61K 31/415 (2006.01) (22) Date of filing: 18.04.2002 A61K 31/445 (2006.01) A61P 25/04 (2006.01) (54) 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS NOCICEPTIN ANALOGS AND ORL1 LIGANDS FOR THE TREATMENT OF PAIN 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ON DERIVATE UND VERWANDTE VERBINDUNGEN ALS NOCICEPTIN ANALOGE UND ORL1 LIGANDEN ZUR BEHANDLUNG VON SCHMERZ DERIVÉS DE LA 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE ET COMPOSÉS SIMILAIRES POUR L’UTILISATION COMME ANALOGUES DU NOCICEPTIN ET LIGANDES DU ORL1 POUR LE TRAITEMENT DE LA DOULEUR (84) Designated Contracting States: • Victory, Sam AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU Oak Ridge, NC 27310 (US) MC NL PT SE TR • Whitehead, John Designated Extension States: Newtown, PA 18940 (US) AL LT LV MK RO SI (74) Representative: Maiwald, Walter (30) Priority: 18.04.2001 US 284666 P Maiwald Patentanwalts GmbH 18.04.2001 US 284667 P Elisenhof 18.04.2001 US 284668 P Elisenstrasse 3 18.04.2001 US 284669 P 80335 München (DE) (43) Date of publication of application: (56) References cited: 23.11.2005 Bulletin 2005/47 EP-A- 0 636 614 EP-A- 0 990 653 EP-A- 1 142 587 WO-A-00/06545 (62) Document number(s) of the earlier application(s) in WO-A-00/08013 WO-A-01/05770 accordance with Art. -
Clonazepam/Ethosuximide 479 Abnormal Movements, and for the Treatment of Panic BNFC Suggests Giving the Following Doses by Slow Intravenous 3
Clonazepam/Ethosuximide 479 abnormal movements, and for the treatment of panic BNFC suggests giving the following doses by slow intravenous 3. Peled R, Lavie P. Double-blind evaluation of clonazepam on pe- injection over at least 2 minutes according to age: riodic leg movements in sleep. J Neurol Neurosurg Psychiatry disorder (see Psychiatric Disorders, below). 1987; 50: 1679–81. For epilepsy and myoclonus treatment is started with • neonates: 100 micrograms/kg, repeated if necessary after 24 4. Saletu M, et al. Restless legs syndrome (RLS) and periodic limb hours movement disorder (PLMD): acute placebo-controlled sleep lab- small doses that are progressively increased to an opti- oratory studies with clonazepam. Eur Neuropsychopharmacol • 1 month to 12 years: 50 micrograms/kg (maximum 1 mg), re- 2001; 11: 153–61. mum dose according to response. Total daily doses peated if necessary may initially be taken in 3 or 4 divided doses; however, 5. Saletu A, et al. On the pharmacotherapy of sleep bruxism: place- Older children may be given the usual adult dose. bo-controlled polysomnographic and psychometric studies with once the maintenance dose has been reached, the daily clonazepam. Neuropsychobiology 2005; 51: 214–25. In children aged over 1 month, these doses by injection may be amount may be given as a single dose at night. In the followed by an intravenous infusion of 10 micrograms/kg per Stiff-man syndrome. Clonazepam has been used as an alter- UK the initial oral dose is 1 mg (500 micrograms in the native to diazepam in the management of stiff-man syndrome hour, adjusted according to response to a maximum of 1 elderly) at night for 4 nights gradually increased over 2 60 micrograms/kg per hour. -
The Iboga Alkaloids
The Iboga Alkaloids Catherine Lavaud and Georges Massiot Contents 1 Introduction ................................................................................. 90 2 Biosynthesis ................................................................................. 92 3 Structural Elucidation and Reactivity ...................................................... 93 4 New Molecules .............................................................................. 97 4.1 Monomers ............................................................................. 99 4.1.1 Ibogamine and Coronaridine Derivatives .................................... 99 4.1.2 3-Alkyl- or 3-Oxo-ibogamine/-coronaridine Derivatives . 102 4.1.3 5- and/or 6-Oxo-ibogamine/-coronaridine Derivatives ...................... 104 4.1.4 Rearranged Ibogamine/Coronaridine Alkaloids .. ........................... 105 4.1.5 Catharanthine and Pseudoeburnamonine Derivatives .. .. .. ... .. ... .. .. ... .. 106 4.1.6 Miscellaneous Representatives and Another Enigma . ..................... 107 4.2 Dimers ................................................................................. 108 4.2.1 Bisindoles with an Ibogamine Moiety ....................................... 110 4.2.2 Bisindoles with a Voacangine (10-Methoxy-coronaridine) Moiety ........ 111 4.2.3 Bisindoles with an Isovoacangine (11-Methoxy-coronaridine) Moiety . 111 4.2.4 Bisindoles with an Iboga-Indolenine or Rearranged Moiety ................ 116 4.2.5 Bisindoles with a Chippiine Moiety ... ..................................... -
The Phytochemistry of Cherokee Aromatic Medicinal Plants
medicines Review The Phytochemistry of Cherokee Aromatic Medicinal Plants William N. Setzer 1,2 1 Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA; [email protected]; Tel.: +1-256-824-6519 2 Aromatic Plant Research Center, 230 N 1200 E, Suite 102, Lehi, UT 84043, USA Received: 25 October 2018; Accepted: 8 November 2018; Published: 12 November 2018 Abstract: Background: Native Americans have had a rich ethnobotanical heritage for treating diseases, ailments, and injuries. Cherokee traditional medicine has provided numerous aromatic and medicinal plants that not only were used by the Cherokee people, but were also adopted for use by European settlers in North America. Methods: The aim of this review was to examine the Cherokee ethnobotanical literature and the published phytochemical investigations on Cherokee medicinal plants and to correlate phytochemical constituents with traditional uses and biological activities. Results: Several Cherokee medicinal plants are still in use today as herbal medicines, including, for example, yarrow (Achillea millefolium), black cohosh (Cimicifuga racemosa), American ginseng (Panax quinquefolius), and blue skullcap (Scutellaria lateriflora). This review presents a summary of the traditional uses, phytochemical constituents, and biological activities of Cherokee aromatic and medicinal plants. Conclusions: The list is not complete, however, as there is still much work needed in phytochemical investigation and pharmacological evaluation of many traditional herbal medicines. Keywords: Cherokee; Native American; traditional herbal medicine; chemical constituents; pharmacology 1. Introduction Natural products have been an important source of medicinal agents throughout history and modern medicine continues to rely on traditional knowledge for treatment of human maladies [1]. Traditional medicines such as Traditional Chinese Medicine [2], Ayurvedic [3], and medicinal plants from Latin America [4] have proven to be rich resources of biologically active compounds and potential new drugs. -
Giới Thiệu Luận Án
Nghiên cứu thành phần hoá học của một số loài cây thuộc họ Betulaceae và họ Zingiberaceae Trương Thị Tố Chinh Trường Đại học Khoa học Tự nhiên Khoa Hóa học Chuyên ngành: Hóa Hữu cơ; Mã số: 62 44 27 01 Người hướng dẫn: 1. GS. TSKH. Phan Tống Sơn 2. PGS TS Phan Minh Giang Năm bảo vệ: 2011 Abstract. Đối tượng nghiên cứu của luận án là 4 loài cây thuộc họ Cáng lò và họ Gừng, là những cây thuộc loại hiếm hoặc mới chỉ được phát hiện gần đây và chưa được nghiên cứu về thành phần hoá học: Tống quán sủi (Alnus nepalensis D. Don), Cáng lò (Betula alnoides Buch. -Ham. ex D. Don), Gừng môi tím đốm (Zingiber peninsulare I. Theilade), Riềng maclurei (Alpinia maclurei Merr.). Kết quả nghiên cứu mới về một số loài thuộc họ Cáng lò và họ Gừng của Việt Nam như sau: Đã xây dựng được qui trình thích hợp để điều chế các phần chiết từ các mẫu của các loài cây được nghiên cứu và các điều kiện phân tách sắc ký để phân lập các hợp chất tinh khiết từ các phần chiết. Lần đầu tiên đã nghiên cứu về thành phần hoá học của cây Tống quán sủi (Alnus nepalensis D. Don) và phân lập được 21 hợp chất; cây Cáng lò (Betula alnoides Buch. -Ham. ex D. Don) và đã phân lập được 16 hợp chất cùng hai hỗn hợp, mỗi hỗn hợp gồm 2 hợp chất; cây Gừng môi tím đốm (Zingiber peninsulare I.