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

Ashraf Brik, John Muldoon, Ying Chuan Lin, John H. Elder, David S. Goodsell, Arthur J. Olson, Valery V. Fokin, K. Bary Sharpless, Chi Huey Wong

Research output: Contribution to journal › Article › peer-review

140 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1246-1248
Number of pages	3
Journal	ChemBioChem
Volume	4
Issue number	11
DOIs	https://doi.org/10.1002/cbic.200300724
Publication status	Published - 7 Nov 2003
Externally published	Yes

Keywords

Click chemistry
Enzyme
HIV protease
Inhibitors
Screening

ASJC Scopus subject areas

Drug Discovery
Organic Chemistry
Biochemistry, Genetics and Molecular Biology(all)

Access to Document

10.1002/cbic.200300724

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

In: ChemBioChem, Vol. 4, No. 11, 07.11.2003, p. 1246-1248.

Research output: Contribution to journal › Article › peer-review

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