Synthesis and antimycobacterial activity of salicylanilides substituted inposition 5

A set of 57 salicylanilides was synthesized, with the substitution being va ried at positions 5, 4', and 3'. The substances were evaluated for antimyco bacterial activity against the strains of Mycobacterium tuberculosis, Mycob acterium kansasii, and Mycobacterium avium. Structure-activity relationship s were determined using the Free-Wilson method, which was further combined with the approach of Hansch. Antimycobacterial activity becomes higher with increasing electron-accepting ability of the substituents on the phenyl ri ng, and with increasing their lipophilicity. The influence of the substitue nts in position 5 is more complex.