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Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide.
The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. Due to the
commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for
the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory
activity and short duration of treatment. In this direction, various heterocyclic compounds have been synthesized and
screened against Mycobacterium tuberculosis. Among them, benzimidazole and imidazole containing derivatives found to
have potential anti-tubercular activity. The present review focuses on various imidazole and benzimidazole derivatives
(from 2015-2019) with their structure activity relationships in the treatment of tuberculosis.
A novel series of 5,5-dimethyl-11-phenyl-4b,5,5a,10,10a,11,11a,12-octahydro-10,11,12-triaza-indeno[2,1-b]fluorenes 3a-3l were prepared by reacting oxindole, aryl amines and acetone using dibutylamine as an organocatalyst via simultaneous Knoevenagel and Michael-type reactions. This preparation is environmentally benign, highly compatible and conveniently carried out in ethanol under mild conditions. The structures of the new compounds were determined by spectroscopic techniques, including IR, 1 H NMR, 13 C NMR and LCHRMS. Docking studies against an enoyl acyl carrier protein reductase predicted that the compounds possessed high binding affinity towards target molecules. The compound 3k (MIC, 40 g/mL) showed comparable activity with Isoniazid at the same concentrations against MT H37 Rv.
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