Mon, 20 Nov 2017

Synthesis, Antimicrobial and Anticancer Studies of Isatin Derivatives of Sparfloxacin

Sirajunisa Talath*1, Bhoomendra A. Bhongade1

1.Department of Pharmaceutical Chemistry, RAK College of Pharmaceutical Sciences, RAKMHSU, POB 11172, Ras Al Khaimah, UAE


ABSTRACT

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 <6.25 µg/mL while the IC50 values against cancer cell lines SW480, HeLa, A549 and HepG2 was in the range of 18.31- >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.

Keywords : Sparfloxacin, Mannich bases, Isatin, Antibacterial, Antitubercular, Anticancer.


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