Heparin derivatives prepared by modification of the uronic acid carboxyl groups

Abstract

Heparin derivatives in which the carboxyl groups of the uronic acid are modified, were synthesized by mild procedures whereby the sulfate groups remained intact. It was found that esterification of the carboxyl group resulted in complete loss of anticoagulant activity. However, heparinyl glycine and heparinyl aminomethanesulfonic acid which contain free acidic groups had considerable effects in prolonging blood clotting. Other bulkier units which may modify the conformation of heparin, or products in which there are no free carboxyl groups had little anti-coagulant effects.