Synthesis and Biological Activities of the Antibiotic B 371 and its Analogs

Abstract

Abstract The synthesis of the title compound 1 is described as well as the syntheses of a series of structural analogs of type 4 . The antimicrobial in vitro activity of these vinyl isocyanides, substituted in β‐position either by an indole derivative or by an aryl or 2‐thienyl group, was tested against Escherichia Coli, Bacillus subtilis , and Mucor muhei TÜ 284 (Table 1). Some of the compounds 4 display higher activity than the naturally occurring parent compound 1 . — A variety of alkyl 2‐isocyanoacrylates of type 5 were included in the biological test. Some of them display exceptionally high antimicrobial activity (Table 2). Upon conversion of the isocyano group into the formamido group ( 4 → 6 ), the biological activity is lost.