PEPTIDYL AMINOSTEROIDS AS POTENTIAL NEW ANTIARRHYTHMIC AGENTS

被引：13

作者：

MOKOTOFF, M

ZHAO, M

MARSHALL, RJ

WINSLOW, E

WONG, LK

LIAO, QJ

机构：

[1] Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA

[2] China Pharmaceutical University, Nanjing

[3] Organon Laboratories, Ltd., Newhouse, Lanarkshire Scotland

来源：

STEROIDS | 1990年 / 55卷 / 09期

关键词：

STEROIDS; PEPTIDYL AMINOSTEROIDS; ANTIARRHYTHMIC AGENTS; POLYMERIC HYDROXYBENZOTRIAZOLE; AMAFALONE; PEPTIDES; AMINOSTEROIDS;

D O I：

10.1016/0039-128X(90)90098-V

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of peptidyl derivatives of the aminosteroid, amafalone (Am), is described. Six analogs were synthesized: the hydrochloride salts of Gly-Am (2) Ala-Gly-Am (3), D-Ala-Gly-Am (4), Pro-Am (6), Pro-Pro-Am (7), and D-Ala-Pro-Am (8). The peptide bonds were formed by the polymeric reagent method using polymeric hydroxybenzotriazole as the activating polymer. Peptidyl aminosteroids 2, 6, 7, and 8, when administered to rats intravenously, had protective antiarrhythmic effects similar to those of amafalone. By the oral route, less marked protection, in comparison to amafalone, was observed with 6, while 7 and 8 were disappointingly inactive.

引用

页码：399 / 404

页数：6

共 14 条

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