a short review on cardiotonic steroids and their aminoguanidine analogues一个简短的回顾强心剂类固醇和氨基胍类似物.pdfVIP

Molecules 2000, 5, 51-81 molecules ISSN 1420-3049 A Short Review on Cardiotonic Steroids and Their Aminoguanidine Analogues Concepción P. Melero*, Manuel Medarde and Arturo San Feliciano Departamento de Química Farmacéutica, Facultad de Farmacia, Campus Miguel de Unamuno, 37007 Salamanca, Spain Tel.: +34 923 29 45 28, Fax: +34 923 29 45 15, E-mail: medarde@gugu.usal.es *Author to whom correspondence should be addressed. Received: 14 November 1999 / Accepted: 9 December 1999 / Published: 21 January 2000 Abstract: A short review on cardiotonic steroids and their analogues is presented. The natu- ral, semisynthetic and synthetic derivatives, as well as their mechanism of action and struc- ture-activity relationships are shown, with a special reference to aminoguanidine deriva- tives. Keywords: Digitalis glycosides analogues, structure-activity relationships, inotropic activ- ity, Na+,K+-ATPase, aminoguanidine analogues. 1. Introduction 3.2.1. Structure-activity relationships 2. Mechanism of inotropic activity 3.2.2. Steroidal framework 2.1. Na+ + 3.2.3 ,K -ATPase . Side chain at C-17 2.2. Isoenzymes 3.2.4. Sugar 3. Compounds displaying inotropic digitalis-like activity 3.2.5. Other substituents at position C-3 3.1. Natural digitalis-like compounds 3.2.6. Pregnane derivatives 3.1.1. Digitalis-like glycosides in vegetal sp