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

摘要

A series of 22 3-aryl substituted-2-(1H(2H)-benzotriazol-1(2)-yl)acrylonitriles was synthesized for a preliminary in vitro evaluation of antitubercular activity according to an international program with the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF). This work reports the synthetic approach and analytical and spectroscopic characterization (UV, IR, 1H- and 13C-NMR) of all compounds synthesized. Several compounds showed an interesting activity in the preliminary screening with a percent growth inhibition of the virulent Mycobacterium tuberculosis between 40 and 99% at the concentration of 12.5 &mgr;g/mL. The most effective derivatives E-5a and E-5e were also tested against M. avium in vitro.