Tuberculosis (TB) remains among the world's great public health challenges. Worldwide resurgence of TB is due to two major problems: the AIDS epidemic, which started in the mid-1980s, and the outbreak of multi-drug resistant (MDR) TB and extensively multi-drug resistant (XMDR). Thus, there is an urgent need for anti-tubercular (anti-TB) drugs with enhanced activity against MDR strains. In recent years, Schiff bases of 1H-indole-2,3-diones arereported to exhibit anti-TB activity. In the current study, Schiff bases of indoline-2,3-dione with the general structure (1  ) were synthesized by the reaction of isatin or its derivatives (1- / 5- / 1,5-substituted isatins) with a series of acid hydrazides in mild conditions. The target Schiff bases were screened for their anti-TB activity against Mycobacterium tuberculosis H37Rv. Compounds with promising and potent anti-TB activity were further screened against single resistant strains of M. tuberculosis and a minimum bacteriostatic (MBC) assay against the pan-sensitive M. tuberculosis H37Rv. Results revealed that these compounds can be strongly recommended as potential candidates as promising leads against resistant strains of M. tuberculosis with MIC and MBC values in the low micromolar range (0.156). A pharmacophore model was developed to further optimize the activity among this series of novel compounds. 

Efficient Schiff bases of indoline-2,3-dione (isatin) derivatives against single resistant strains of Mycobacterium tuberculosis

246th National Meeting (2013)

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