1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study.

Abstract:

:1,3-dihydro-2H-indol-2-ones derivatives are reported to exhibit a wide variety of biodynamic activities such as antituberculer, anti HIV, fungicidal, antibacterial, anticonvulsant. These valid observations led us to synthesize some new indole-2-one derivative. Thus, herein we report synthesis of various 5-substituted-3-[{5-(6-methyl-2-oxo/thioxo-4-phenyl-1,2,3,4 tetrahydro pyrimidin-5-yl)-1,3,4-thiadiazol-2-yl}imino]-1,3-dihydro-2H-indol-2-one derivatives 4a-l using one pot multicomponent-Biginelli reaction via CaCl(2) catalyst. Structures and purity of these compounds were confirmed by elemental, IR, ((1)H &(13)C) NMR and Mass spectral analysis. Newly synthesized compounds were also tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H(37)Rv, in vitro antibacterial activity against selected human pathogens viz. Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Staphylococcus aureus, Staphylococcus pyogenus, Bacillus subtilis and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus clavatus strains.

journal_name

Eur J Med Chem

authors

Akhaja TN,Raval JP

doi

10.1016/j.ejmech.2011.09.023

subject

Has Abstract

pub_date

2011-11-01 00:00:00

pages

5573-9

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00683-0

journal_volume

46

pub_type

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