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Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease.

ABSTRACT: A series of trifluoromethyl ketones as SARS-CoV 3CL protease inhibitors was developed. The inhibitors were synthesized in four steps from commercially available compounds. Three different amino acids were explored in the P1-position and in the P2-P4 positions varying amino acids and long alkyl chain were incorporated. All inhibitors were evaluated in an in vitro assay using purified enzyme and fluorogenic substrate peptide. One of the inhibitors showed a time-dependent inhibition, with a K(i) value of 0.3 microM after 4h incubation.

SUBMITTER: Shao YM 

PROVIDER: S-EPMC7127754 | biostudies-literature | 2008 Apr

REPOSITORIES: biostudies-literature

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Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease.

Shao Yi-Ming YM   Yang Wen-Bin WB   Kuo Tun-Hsun TH   Tsai Keng-Chang KC   Lin Chun-Hung CH   Yang An-Suei AS   Liang Po-Huang PH   Wong Chi-Huey CH  

Bioorganic & medicinal chemistry 20080215 8

A series of trifluoromethyl ketones as SARS-CoV 3CL protease inhibitors was developed. The inhibitors were synthesized in four steps from commercially available compounds. Three different amino acids were explored in the P1-position and in the P2-P4 positions varying amino acids and long alkyl chain were incorporated. All inhibitors were evaluated in an in vitro assay using purified enzyme and fluorogenic substrate peptide. One of the inhibitors showed a time-dependent inhibition, with a K(i) va  ...[more]

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