Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry
ISSN: 0975-413X
Abstract
Synthesis, characterization and biological evaluation of pyrazolones containing multi substituted thiazolidinones and oxadizoles
Author(s): K. Kishore Kumar, K. B. Chandrashekar, G. Nagaraju, G. Madhu,Y. N. Spoorthy and L. K. Ravindra NathA series of novel Pyrazolone Schiff bases bearing thiazolidinone and oxadiazoles systems were prepared from ethyl- 2-(4-formyl-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)acetate (4) and substituted amines. All pyrazolone schiff bases were refluxed with mercapto acetic acid in presence of anhydrous zinc chloride and solvent N,N-dimethyl formamide to afforded novel series of Ethyl-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)-3-methyl-5-oxo- 4,5-dihydro-1H-pyrazol-1-yl)acetate [5a-f]. Novel moieties 2-(1-((4-acetyl-5-(4-substituted phenyl)-5-methyl-4,5- dihydro-1,3,4-oxadiazol-2-yl) methyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-yl)-3-(4-substituted phenyl) thiazolidin-4-one were synthesized by the condensation of (E)-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)- 3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-N'-(1-(4-substitutedphenyl)ethylidene)acetohydrazide (6a-f) and substituted ketones (7a-e) afford corresponding (E)-2-(4-(3-(4-substitutedphenyl)-4-oxothiazolidin-2-yl)-3-methyl-5- oxo-4,5-dihydro-1H-pyrazol-1-yl)-N'-(1-(4-substitutedphenyl) ethylidene)acetohydrazide (8a-f). This was subjected to cyclization with excess of acetic anhydride to give corresponding congeners 2-(1-((4-acetyl-5-(4- substitutedphenyl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4- yl)-3-(4-substitutedphenyl) thiazolidin-4-one (9a-j) in excellent yields. The structures of these newly synthesized compounds were characterized by 1H-NMR, 13C-NMR, Mass, IR and elemental analysis. The prepared compounds have been screened on some strains of bacteria and fungi.
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