In vitro evaluation of tetrazoles as a novel class of Antimycobacterium tuberculosis agents

• Main Authors: Bhaskar V.H., Mohite P.B .
• Format: Article
• Language: English
• Published: Tabriz University of Medical Sciences 2012-06-01
• Series: Advanced Pharmaceutical Bulletin
• Subjects: Azatidinones; Tetrazole; Antimycobacterial activity; TAACF
• Online Access: http://apb.tbzmed.ac.ir/Portals/0/Archive/Vol2No1/5.Popat-Mohite.pdf

Purpose: We report here the antimycobacterial activity of some already synthesized tetrazole derivatives containing tetrazole against Mycobacterium tuberculosis strain H37Rv. Methods: In vitro evaluation of the antitubercular activity was carried out within the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) screening program for the discovery of novel drugs for the treatment of tuberculosis. Under the direction of the US National Institute of Allergy and Infectious Diseases (NIAID), Southern Research Institute that coordinates the overall program. The method of TAACF was followed for evaluation of activity. Results: This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituent’s present in azatidinone core. Compounds having a 4-MeOC6H4 4-N(CH3)2C6H4 group as the substituent on β-lactam ring were active. The highest activity was registered for compounds having 4-MeOC6H4 as substituent. Conclusion: The new compounds showed high potency and promising antitubercular activity and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents.