期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 5, 页码 1564-1571出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.003
关键词
3,5-Dicarbamoyl-1,4-dihydropyridines; N-Arylacetoacetamides; Antibacterial activity; Antitubercular activity; Antimycobacterial activity
资金
- University Grants Commission (UGC), New Delhi, India
A novel class of 4-aryl/heteroaryl-2,6-dimethyl-3,5-bis-N-(phenyl/substituted phenyl)-carbamoyl-1,4-dihydropyridines has been synthesized by simple, economical and eco-friendly, modified Hantzsch condensation reaction making use of N-arylacetoacetamides, aryl or heteroaryl aldehydes and ammonium acetate. The newly synthesized compounds were characterized by their spectral (IR, H-1 NMR, Mass), elemental analyses data and evaluated for in vitro antitubercular activity against Mycobacterium tuberculosis H(37)Rv ATCC 27294 and antibacterial activity against different Gram +ve and Gram -ve bacteria. The preliminary screening results revealed that some of the compounds possess promising antimicrobial activity. Amongst the new series of compounds, 6m containing pyrrolyl and 4-methyl-phenyl groups and 6r possessing 2-pyridyl and 2-methylphenyl groups were found to exhibit a significant antitubercular activity (MIC = 12.5-25 mu g/mL) in comparison with the first line drug pyrazinamide. (C) 2011 Elsevier Masson SAS. All rights reserved.
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