Synthesis and antitubercular activity of 3-aryl substituted-2-(1H(2H) benzotriazol-1(2)-yl)acrylonitriles

A series of 22 3-aryl substituted-2-(1H(2H)-benzotriazol-1(2)-yl)acrylonitr iles was synthesized for a preliminary in vitro evaluation of antitubercula r activity according to an international program with the Tuberculosis Anti microbial Acquisition & Coordinating Facility (TAACF). This work reports th e synthetic approach and analytical and spectroscopic characterization (UV, IR, H-1- and C-13-NMR) of all compounds synthesized. Several compounds sho wed an interesting activity in the preliminary screening with a percent gro wth inhibition of the virulent Mycobacterium tuberculosis between 40 and 99 % at the concentration of 12.5 mu g/mL. The most effective derivatives E-5a and E-5e were also tested against M. avium in vitro. (C) 2000 Editions sci entifiques et medicales Elsevier SAS.