Rapid Diversity-Oriented Synthesis in Microtiter Plates for In Situ Screening of HIV Protease Inhibitors

Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar...

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Bibliographic Details
Published in:Chembiochem : a European journal of chemical biology 2003-11, Vol.4 (11), p.1246-1248
Main Authors: Brik, Ashraf, Muldoon, John, Lin, Ying-Chuan, Elder, John H, Goodsell, David S, Olson, Arthur J, Fokin, Valery V, Sharpless, K. Bary, Wong, Chi-Huey
Format: Article
Language:English
Subjects:
click chemistry
Combinatorial Chemistry Techniques
enzyme
HIV protease
HIV Protease - chemistry
HIV Protease - genetics
HIV Protease Inhibitors - chemical synthesis
HIV Protease Inhibitors - chemistry
HIV-1 - enzymology
Hydrogen Bonding
inhibitors
Molecular Structure
Mutation
Peptide Library
screening
Structure-Activity Relationship
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Summary:Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.
ISSN:1439-4227
1439-7633
1439-4227
DOI:10.1002/cbic.200300724