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Rapid Diversity‐Oriented Synthesis in Microtiter Plates for In Situ Screening of HIV Protease Inhibitors
Author(s) -
Brik Ashraf,
Muldoon John,
Lin YingChuan,
Elder John H.,
Goodsell David S.,
Olson Arthur J.,
Fokin Valery V.,
Sharpless K. Bary,
Wong ChiHuey
Publication year - 2003
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200300724
Subject(s) - click chemistry , protease , microtiter plate , in situ , triazole , human immunodeficiency virus (hiv) , chemistry , hiv 1 protease , mutant , combinatorial chemistry , enzyme , biochemistry , biology , chromatography , virology , organic chemistry , gene
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.