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/).
A series of pyrano [2,3-b]indoles, was efficiently synthesized via one-pot, multi component reaction (MCRs) of 1,3-bifunctional synthon(malononitrile/ethylcyano acetate), aromatic aldehydes and oxiindole in the presence of various basic catalyst. The key advantages of this process are high yields, shorter reaction times, easy work-up, and purification of products by non-chromatographic method.
The synthesis of a novel dihydropyridine, bearing carbethoxy groups at C(3) and C(5), respectively, has been achieved by applying three component Hantzsch-type condensation. The products were assayed for their in vitro biological assay antibacterial activity against with two Gram-positive bacteria Staphylococcus aureus MTCC-96, Streptococcus pyogenes MTCC 443, two Gram-negative bacteria Escherichia coli MTCC 442, Pseudomonas aeruginosa MTCC 441 and three fungal strains Candida albicans MTCC 227, Aspergillus Niger MTCC 282, Aspergillus clavatus MTCC 1323 taking ampicillin, chloramphenicol, ciprofloxacin, norfloxacin, nystatin, and griseofulvin as standard drugs.
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