Semisynthesis of A23187 (calcimycin) analogs. II. Introduction of a methyl group on the benzoxazole ring.

Abstract

Semisynthesis of two demethylamino A23187 with a methyl group in the 4- or 5-position on the benzene ring were carried out via the cleavage of A23187 oxazole ring and rebuilding of modified benzoxazoles. These compounds were shown to release Ca++ and MG++ from mitochondria and to keep part the antibacterial activity of the natural metabolite.