A small library of compounds are synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37RV. Two compounds, -[(2 0 ,4 0 -dinitrophenyl) sulphonyl]-4-(p-aminophenylsulphonylamino)-6-(2 0 -chlorophenyl)-pyrimidine-5-carboxamide F b and 2-hydrazino-4-(p-aminophenylsulphonylamino)-6-(2 0 -chlorophenyl)-pyrimidine-5-carboxamide D b were found to be the most active compounds in vitro with MIC of 0.02 lg/mL against MTB and were more potent compared to isoniazid (MIC: 0.03 lg/mL). ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
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.
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 vitro anti 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.
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 Aa-h.. The newly synthesized compounds were characterized by elemental analyses, infrared (IR), 1H NMR and 13C NMR spectroscopic investigation.
Series of 2-mercapto-4-(p-aminophenylsulphonylamino)-6-(aryl)-pyrimidine-5-carboxamide A a-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), 1 H NMR and 13 C NMR spectroscopic investigation.
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