Synthesis and antimicrobial activity of 1-(benzo[b]thiophen-4-yl)-4-(2-(oxo, hydroxyl, and fluoro)-2-phenylethyl)piperazine and 1-(benzo[d]isothiazole-3-yl)-4-(2-(oxo, hydroxy, and fluoro)-2-phenylethyl)piperazine derivatives

Authors : Vaibhav MISHRA, Tejpal Singh CHUNDAWAT

Pages : 713-729

View : 17 | Download : 6

Publication Date : 0000-00-00

Article Type : Research Paper

Abstract :Twenty-two compounds in a series of 1-insert ignore into journalissuearticles values(benzo[$b$]thiophen-4-yl);-4-insert ignore into journalissuearticles values(2-insert ignore into journalissuearticles values(oxo, hydroxy, and fluoro);-2-phenylethyl); piperazine and 1-insert ignore into journalissuearticles values(benzo[$d$]isothiazole-3-yl);-4-insert ignore into journalissuearticles values(2-insert ignore into journalissuearticles values(oxo, hydroxy, and fluoro);-2-phenylethyl);-piperazine derivatives were synthesized through nucleophilic substitution reaction of phenacyl bromides with hetero arylpiperazine, reduction, and then fluorination. Compound K2 showed potent activity against gram-negative bacterial stain P. aeruginosa with minimum inhibitory concentration insert ignore into journalissuearticles values(MIC); value of 12.5 μg/mL. This compound showed better inhibitory activity than the standard drug chloramphenicol. K4 against S. aureus, H2 against P. aeruginosa, and F4 against E. coli showed good inhibitory activity with MIC values of 62.5 μg/mL. Compounds K1, K2, K4, K8, F1, and F3 showed good inhibitory activity against fungal stain C. albicans with MIC values of 250 μg/mL. The crystal structure of F1 was determined by single-crystal XRD insert ignore into journalissuearticles values(CCDC 1832090);.
Keywords : Piperazine, benzo b thiophene, benzo d isothiazole, synthesis, antimicrobial, crystal structure