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

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 benzothiadiazine 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 μg/mL) is also discussed. A new series of benzothiadiazine 1,1-dioxide based congeners was synthesized and evaluated against Mycobacterium tuberculosis, Gram-positive, Gram-negative bacteria and fungi. Further, in vivo activity of earlier potent molecule of this series is also discussed. [Display omitted]