Synthesis, Antimicrobial and cytotoxic activity of New Heterocyclic Hybrids Based on 2,5-Dimethylpyrrole and Pyrrole Scaffolds

被引:5
作者
Joshi, S. D. [1 ]
More, U. A. [1 ]
Kulkarni, V. H. [1 ]
机构
[1] SETs Coll Pharm, Dept Pharmaceut Chem, Dharwad 580002, Karnataka, India
关键词
Pyrroles; acid hydrazide derivatives; antibacterial activity; antitubercular activity; antifungal activity; broth dilution assay method; cytotoxicity; ACID HYDRAZIDE ANALOGS; POTENTIAL ANTIBACTERIAL; ANTICANCER ACTIVITY; RING-SYSTEMS; DERIVATIVES; ANTIFUNGAL; OXADIAZOLE; TRIAZOLE; DESIGN;
D O I
10.4103/0250-474X.117439
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A series of 4-(2,5-dimethylpyrrol-1-yl)/4-pyrrol-1-yl benzoic acid hydrazide analogs, some derived triazoles, azetidinones, thiazolidinones, and pyrroles have been synthesized in good yields and structures of these compounds were established by IR, H-1 NMR, C-13 NMR, mass spectral, and elemental analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal, and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by the broth dilution assay method. Twenty one of these compounds displayed good antimicrobial activity, with a MIC value of 1-4 mu g/ml. Several compounds 4c, 8-10, 15b-15h, and 16b-16d exhibited good in vitro antitubercular activity with MIC value 1-2 mu g/ml. Further, some title compounds were also assessed for their cytotoxic activity (IC50) against mammalian Vero cell lines and A(549) (lung adenocarcinoma) cell lines using the MTT assay method. The results revealed that these compounds exhibit antitubercular activity at non-cytotoxic concentrations.
引用
收藏
页码:310 / 323
页数:14
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