New lydiamycin cyclodepsipeptides useful for controlling diseases cause by mycobacteria, e.g. tuberculosis and leprosy

摘要

Lydiamycin cyclodepsipeptides (I) are new. Lydiamycin cyclodepsipeptides of formula (I) are new. R1 : H, 1-12C alkyl, optionally substituted (hetero)aralkyl, CORa, CSRa, 3-10C (hetero)cycloalkyl or optionally substituted (hetero)aryl; Ra : H or 1-12C alkyl optionally substituted with COOH, OH or NH2; R2 : H or oxo; R3 : H, OH, oxo, 1-12C alkyl, CORa, CSRa, OCORa, OCSRa or OCOORa; R4 : H; R1+R2, R3+R4 : double bonds; R5 : H, 1-12C alkyl, optionally substituted (hetero)aralkyl, CORa, CSRa, OCORa, OCSRa or OCOORa. An independent claim is also included for a process for producing (I). [Image] ACTIVITY : Antibiotic; Tuberculostatic; Antileprotic. Lydiamycin A had MIC values (mu g/ml) of 25 against Mycobacterium smegmatis, 3.1 against Mycobacterium vaccae and 6.3 against Mycobacterium aurum MECHANISM OF ACTION : None given.