Синтез, противогрибковая и противовирусная активность N-бензильных производных тетраенового макролидного антибиотика люцензомицина

Reactions of the tetraene macrolide antibiotic lucensomycin with p -substituted aromatic aldehydes and sodium cyanoborohydride under conditions of the reaction of reductive amination resulted in formation of N-benzyl derivatives. Physicochemical, medical, and biological properties of the obtained derivatives of lucensomycin were studied. Biological investigations showed that N-benzyl derivatives of lucensomycin were low-toxicity agents and exhibited high antifungal and antiviral activity. The pharmacological tests showed that the acute toxicity (LD 50 ) of the obtained derivatives of lucensomycin was 6 times as low as that of the initial antibiotic.