4.7 Article

Anti-tubercular agents. Part 5: Synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 10, Pages 4545-4553

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.07.015

Keywords

Anti-tubercular agents; Benzothiadiazine 1,1-dioxides; M tuberculosis; MDR-and XDR-TB

Funding

  1. Department of Science Technology, New Delhi [DST: SR/S1/OC-42/2008]
  2. CSIR, New Delhi

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In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzo-thiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and in vivo study of recently reported potent molecule 4 (MIC = 1 mu g/mL) is also discussed (C) 2010 Elsevier Masson SAS. All rights reserved.

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