Document Detail

Enamino-oxindole HIV protease inhibitors.
MedLine Citation:
PMID:  22749283     Owner:  NLM     Status:  MEDLINE    
We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2' subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar K(i) and antiviral IC(50) in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Michael Eissenstat; Tanya Guerassina; Sergei Gulnik; Elena Afonina; Abelardo M Silva; Douglas Ludtke; Hiroko Yokoe; Betty Yu; John Erickson
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Publication Detail:
Type:  Journal Article     Date:  2012-06-07
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  22     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2012 Aug 
Date Detail:
Created Date:  2012-07-20     Completed Date:  2012-11-30     Revised Date:  2013-06-03    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  5078-83     Citation Subset:  IM    
Copyright Information:
Copyright © 2012 Elsevier Ltd. All rights reserved.
Sequoia Pharmaceuticals, Inc., Gaithersburg, MD 10878, USA.
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MeSH Terms
Binding Sites
Crystallography, X-Ray
Drug Resistance, Viral / drug effects
HIV Protease / chemistry*,  metabolism
HIV Protease Inhibitors / chemical synthesis,  chemistry*,  pharmacology
HIV-1 / drug effects,  enzymology*
Indoles / chemical synthesis,  chemistry*,  pharmacology
Protein Structure, Tertiary
Structure-Activity Relationship
Sulfonamides / chemistry,  pharmacology
Reg. No./Substance:
0/HIV Protease Inhibitors; 0/Indoles; 0/Sulfonamides; 0/oxindole; EC 3.4.23.-/HIV Protease; YO603Y8113/darunavir

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