Antitubercular

Isatin is an endogeneous and an important class of heterocyclic compound. It possess indole nucleus having both keto and lactam moiety with a diverse pharmacological properties like antimicrobial, antitubercular, anticonvulsant activity etc. Isatin derivatives are synthetically important substrates, which can be used for the synthesis of a large variety of heterocyclic compounds, and as raw material for drug synthesis. Recently, isatin derivatives have attracted strong interest in organic and medicinal chemistry due to their potent biological and pharmacological activities. The purpose of this review is to provide information on the pharmacological activities of isatin and its derivative.

Mannich bases of sparfloxacin were synthesized from the reaction of 5-acetylamino-1-cyclopropyl-7-(3΄,5΄-dimethyl-piperazin-1-yl)-6,8-difluoro-4-oxo1,4-dihydro-quinoline-3-carboxylic acid with formaldehyde and several isatin derivatives. The structures of the synthesized compounds were elucidated from the IR, 1H NMR, 13C NMR and FAB Mass data. The synthesized compounds were evaluated for the antibacterial, antitubercular and anticancer activity. The compounds showed good activity against Gram-positive bacteria and moderate activity against tested Gram-negative bacteria. The MIC for the compounds against M. tuberculosis H37Rv strain was 50 µg/mL. The most potent compound in this series 3c exhibited enhanced antibacterial activity than sparfloxacin against S. aureus, Bacillus Sp while the anticancer activity was in the range of 18.31- 23.61 µg/mL.