Design, synthesis, and evaluation of trifluoromethyl ketones as inhibitors of SARS-CoV 3CL protease
Resource
Bioorganic & Medicinal Chemistry 16 (8): 4652-4660
Journal
Bioorganic & Medicinal Chemistry
Pages
4652-4660
Date Issued
2008
Date
2008
Author(s)
Shao, Yi-Ming
Yang, Wen-Bin
Kuo, Tun-Hsun
Tsai, Keng-Chang
Lin, Chun-Hung
Yang, An-Suei
Liang, Po-Huang
Wong, Chi-Huey
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.
SDGs
File(s)![Thumbnail Image]()
Loading...
Name
13.pdf
Size
359.98 KB
Format
Adobe PDF
Checksum
(MD5):77fe4b11fc1197e030186d33305af14e