| 摘要 |
α-Chymotrypsin inhibitors of thiourea class are reported that could be potent inhibitors of proteases, elastases, proteasomes, NS3 and NS4 serine protease of hepatitis C virus, dengue virus, etc. Compounds 1-22, which are belong to thiourea class, showed good inhibition. Their kinetics study and cytotoxicity profiles showed all type of inhibition except uncompetitive-type inhibition and no cytotoxicity except few compounds. Competitive type of inhibitors could inhibit other α-chymotrypsin-like serine proteases, which are therapeutics target. |
| 主权项 |
1. An inhibitor of alpha chymotrypsin comprising a compound of structure:where, R1=R4=H, R2=3-chlorophenyl, and R3=4-chlorophenyl, 3,4-dichlorophenyl, 3-chlorophenyl, 3-methoxyphenyl, 2-methoxyphenyl, 4-methoxyphenyl, 5-chloro-2-methylphenyl, 2,4-dichlorophenyl, p-tolylthiourea, m-tolylthiourea, 3,4-difluorophenyl, 4-fluorophenyl, 2,3-dichlorophenyl, 2,5-dimethylphenyl, 2,4-dimethylphenyl, 2,6-dichlorophenyl, o-tolylthiourea, pyridin-4-ylmethyl, pyridin-3-yl, andwhere, R1=R4=H, R2=3-phenylthiourea, and R3=4-bromophenyl, 3-bromophenyl, 2,4-bifluorophenyl. |
