Analogs of Tirandamycin

Abstract

The purpose of this SIP was to chemically modify the antibiotic tirandamycin in order to increase either its spectrum of activity or its potency. The cyc1ohexy1 amide of tirandamycic acid was prepared. Based on the work done by Mager1ein, tirandamycy1 chloride was condensed with various 1,3-dicarbony1 compounds. In addition, condensation was tried with other activated methylene compounds such as ethyl cyanoacetate, ma1ononitri1e and dimethyl methy1phosphonate.