Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 78, Issue -, Pages 207-216Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.02.015
Keywords
Multicomponent reaction; 5-Imidazopyrazole incorporated polyhydroquinolines; Antimicrobial activity; Antituberculosis activity; Antimalarial activity
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Funding
- University Grants Commission - New Delhi, India
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A new category of polyhydroquinoline derivatives 8a-t were synthesized in moderate to good yield (64-85%) by one-pot three-component cyclocondensation reaction of 5-(1H-imidazol-1-yl)-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde 3 with various enaminones 6a-h and different active methylene compounds (malononitrile 7a, ethylcaynoacetate 7b and caynoacetamide 7c) in absolute ethanol. The newly synthesized compounds were evaluated for their in vitro antimalarial activity against Plasmodium falciparum, in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi and also for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain. Two of them (8n, 8t) exhibited excellent antimalarial activity. Some of them exhibited excellent antibacterial activity and moderate antituberculosis activity compared with the first line drugs. (C) 2014 Elsevier Masson SAS. All rights reserved.
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