| Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats. | |
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MedLine Citation:
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PMID: 21920742 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed its instability in rat plasma. A hypothesis for this liability was proposed, and strategies to overcome this issue were pursued, leading to discovery of highly potent 40 and 41, which featured dramatically improved rat PK profiles. |
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Authors:
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Maosheng Duan; Wieslaw M Kazmierski; Pek Y Chong; Felix Deanda; Mark Edelstein; Rob Ferris; Jennifer Peckham; Pat Wheelan; Zhiping Xiong; Huichang Zhang; Rena Nishizawa; Yoshikazu Takaoka |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-8-23 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Aug |
Date Detail:
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Created Date: 2011-9-16 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Infectious Disease Medicine Discovery & Development, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27706, USA. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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