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  • Chem Sci Trans., 2013, 2(3),  pp 1056-1062  

    DOI:10.7598/cst2013.490

    Research Article

    Design and Synthesis of Novel 2-Trichloromethyl-4-Substituted Quinazoline Derivatives as Anti-tubercular Agents

  • MANEESH KUMAR SRIVASTAV and S. M. SHANTAKUMAR*
  • Department of Pharmaceutical Chemistry, V. L. College of Pharmacy, Raichur-584103, Karnataka, India
  • Abstract

    In order to produce a new lead for anti-tubercular drug a series of novel 2-trichloromethyl quinazoline derivatives bearing substituted secondary amine group at the 4th position were designed, synthesized and evaluated for their in vitro anti-tubercular activity against bacterial strain of M. tuberculosis H37Rv ATCC (American Type Culture Collection) by Alamar Blue assay method (MABA). The targeted molecules (4a-j) were synthesized from 4-chloro-2-(trichloromethyl) quinazoline and substituted secondary amine in dichloromethane using catalytic amount of KI, under reflux for 15-18 h. All the targeted compounds are new chemical entities and obtained in satisfactory yields and the structure of the synthesized compounds are in agreement with spectral data. Compound 4a and 4f exhibited potent anti-tubercular activity against bacterial strain of M. tuberculosis H37Rv, with MIC value 6.25 μG.

    Keywords

    Anti-tubercular activity, 2-Trichloromethyl quinazoline, Acetylation

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