Journal of Medicinal Chemistry p. 666 - 669 (1980)
Update date:2022-08-02
Topics:
Johnson, Rodney L.
The following N-(α-hydroxyalkanoyl) derivatives of Leu-Val-Phe-OCH3 were synthesized and tested for their ability to inhibit human amniotic renin: D- and L-α-hydroxyisocaproyl-Leu-Val-Phe-OCH3, D- and L-α-hydroxyisovaleryl-Leu-Val-Phe-OCH3, L-2-hydroxy-3-phenylpropanoyl-Leu-Val-Phe-OCH3, and D- and L-α-hydroxyphenylacetyl-Leu-Val-Phe-OCH3.Analysis of the compounds through the use of Dixon plots showed all of the compounds to be competitive inhibitors of renin.All but D-α-hydroxyisovaleryl-Leu-Val-Phe-OCH3 were found to be more active than the known tetrapeptideinhibitor Leu-Leu-Val-Phe-OCH3 (1).The two most active compounds of the series were L-α-hydroxyisocaproyl-Leu-Val-Phe-OCH3 (Ki = 0.23 mM) and L-α-hydroxyisovaleryl-Leu-Val-Phe-OCH3 (Ki = 0.3 mM).
View MoreShanghai Massive Chemical Technology Co., Ltd.
website:http://www.massivechem.com/
Contact:+86 21 34943721
Address:Room 435, 4th floor, Building 9, No. 2568 Gudai Road,Minhang District, Shanghai,
Chengdu Boon Stream Chemical Industry Co.,Ltd.
Contact:+86-28-83156758
Address:No.859,Dongzikou Road,Jinniu District,Chengdu,Sichuan,P.R.China
Shanghai Hohance Chemical Co., ltd
Contact:13914753421
Address:Fl.5;Bld. 70, Lane 1500; Xinfei Road
NINGBO YINZHOU PRECISE COLOR CO.,LTD.
Contact:86-574-88139809 86-574-83033159
Address:Qiming Road,Yinzhou,Ningbo,China
Contact:+1-973-357-0577
Address:10 Taft Rd.
Doi:10.1016/S0040-4039(03)00224-7
(2003)Doi:10.1002/pola.24572
(2011)Doi:10.1016/S0040-4039(01)95424-3
(1979)Doi:10.1039/P29800000260
(1980)Doi:10.1021/ja961010w
(1996)Doi:10.1081/SCC-120027232
(2004)