1-Phenylpyrazolo[3,4-dlpyrimidines:Structure-Activity Relationships for C6 Substituents at A1 and A2a Adenosine Receptors

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Title 1-Phenylpyrazolo[3,4-dlpyrimidines:Structure-Activity Relationships for C6 Substituents at A1 and A2a Adenosine Receptors
Author Chebib, Mary; McKeveney, Declan; Quinn, Ronald J
Journal Name Bioorganic & Medicinal Chemistry
Year Published 2000
Place of publication UK
Publisher Pergamon
Abstract Substitution of 1-phenylpyrazolo[3,4-d]pyrimidines at C6 with N-alkyl-2-thiopropionamide groups has resulted in a series of 18 compounds which have been evaluated for binding at A1 and A2A adenosine receptors. Introduction of an N-ethyl group gave increased affinity at both A1 and A2A receptors for the amino compound 7b compared to the primary amide 7a. An additional hydrophobic pocket exists for substituents on the amide. This pocket allows an N-ethyl group for increased affinity at both A1 and A2A receptors, allows larger alkyl groups at A2A receptors but not at A1 receptors and there is an H-bond interaction requiring one H-bond donor. Molecular modeling studies have also enabled a proposal of the amino acid residues involved in ligand binding at both the A1 and A2A receptors.
Peer Reviewed Yes
Published Yes
Publisher URI http://www.elsevier.com/wps/find/journaldescription.cws_home/129/description#description
Copyright Statement Copyright 2000 Elsevier : Reproduced in accordance with the copyright policy of the publisher : This journal is available online - use hypertext links.
Volume 8
Page from 2581
Page to 2590
ISSN 0968-0896
Date Accessioned 2001-01-01
Date Available 2007-03-13T21:53:31Z
Language en_AU
Research Centre Eskitis Institute for Drug Discovery
Subject Science & Technology
URI http://hdl.handle.net/10072/3145
Publication Type Article in Scholarly Refereed Journal
Publication Type Code c1

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