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2 International Letters of Chemistry, Physics and Astronomy

2 2014

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Synthesis, Characterization and Biological evaluation of some newer 5-[6-chloro/fluoro/nitro-2-(p-chloro/ fluoro/ methyl phenyl)-quinolin-4-yl]-1,3,4-oxadiazole-2-thiols

100%

Faldu V. J. , Talpara P. K. , Bhuva N. H. , Vachharajani P. R. , Shah V. H.

International Letters of Chemistry, Physics and Astronomy

2014

tom Vol. 6

26--32

Recent study shows that quinolines represent one of the most active classes of compounds possesses wide spectrum biodynamic activities and use as potent therapeutic agents. In present research work, 5-[6-chloro/fluoro/nitro-2-(p-chloro/fluoro/methyl phenyl)-quinolin-4-yl]-1,3,4-oxadiazole-2-thiols have been synthesized by condensation of substituted quinoline-4-carbohydrazides and mixture of carbon disulphide and potassium hydroxide. All of these compounds were screened for their in vitroanti microbial assay against gram (+ve), gram (-ve) bacteria and fungi activity compared with standard drugs viz., Ampicilin, Chloramphenicol, Ciprofloxacin, Norfloxacin, Griseofulvin and Nystatin at different concentrations.

Synthesis of novel 2-mercapto-4-(p-aminophenyl sulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide derivatives via the Biginelli reaction

86%

Bhuva N. H. , Gothalia V. K. , Singala P. M. , Talpara P. K. , Faldu V. J. , Shah V. H.

International Letters of Chemistry, Physics and Astronomy

2014

tom Vol. 17, iss. 2

168--173

Series of 2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide Aa-h were synthesized via the biginelli condensation. 2-mercapto-4-amino-6-(aryl)-pyrimidine-5-carboxamide react with p-acetamidophenylsulphonylchloride in the presence of pyridine 2 to form 2-mercapto-4-(p-acetamidophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide 3. It was treated with diluted HCl under reflux afforded 2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide A a-h. The newly synthesized compounds were characterized by elemental analyses, infrared (IR), 1H NMR and 13 C NMR spectroscopic investigation.