Synthesis, characterization and pharmacological screening of some novel 5-imidazopyrazole incorporated polyhydroquinoline derivatives.

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ID: 74074
2014
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Abstract
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.
Reference Key
kalaria2014synthesiseuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Kalaria, Piyush N;Satasia, Shailesh P;Raval, Dipak K;
Journal European journal of medicinal chemistry
Year 2014
DOI
10.1016/j.ejmech.2014.02.015
URL
Keywords
Antimicrobial activity multicomponent reaction antimalarial activity 5-imidazopyrazole incorporated polyhydroquinolines antituberculosis activity

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