Tetrahedron p. 4199 - 4214 (1996)
Update date:2022-08-03
Topics:
Occhiato, Ernesto
Jones, J. Bryan
Various enantiomeric amine and aminoalcohol amide and α-ketoamide derivatives have been evaluated as competitive inhibitors of the representative serine proteases α-chymotrypsin (CT) and subtilisin Carlsberg (SC). Each compound studied was an effective competitive inhibitor of both enzymes. However, only for the best inhibitor, N-pyruvoyl-1-(1-naphthyl)ethylamine (K1 27 μM for the S-enantiomer with CT), was noteworthy enantiomeric discrimination manifest, with the S-enantiomer being a significantly more powerful inhibitor of CT and SC than its R-counterpart by factors of 12.6- and 73-fold, respectively. The enzyme-inhibitor interactions responsible for this strong binding and enantiomeric discrimination were revealed by molecular modelling analyses.
View MoreRizhao Lanxing Chemical Indusrial Co.,Ltd
Contact:86-633-2616708
Address:NO.15 West road Shenglan, Lanshan district, Rizhao City
Jiangsu Cale New Material Co.ltd
Contact:+86-515-88334667/88203550
Address:Zhongshan 3rd Road, Coastal Chemical Industry Park, Yancheng, Jiangsu, China
Huangshi Meifeng Chemical Co.,ltd.
Contact:+86-714-6516706
Address:1941-4-3#,Hubin Avenue,Huangshi,Hubei,China
Liaoyang Xinyou Chemical Products Co.,Ltd.
Contact:+86-419-5165433 13604191870
Address:Huishang Road6-1, Hongwei District, Liaoyang, Liaoning, China
Huangshi Shennong Chemical Technology Co., Ltd
Contact:+86-714-3072290
Address:Eastern industrial park , Tieshan district , Huangshi city ,Hubei province , China
Doi:10.1021/jo01017a056
(1965)Doi:10.1039/p19960000593
(1996)Doi:10.1016/S0031-9422(00)84340-X
(1971)Doi:10.1016/0022-328X(83)80182-X
(1983)Doi:10.1021/jo952165+
(1996)Doi:10.1021/ic9515416
(1996)