Oxadiazolo pyrrolidine carboxamides as enoyl-ACP reductase inhibitors: design, synthesis and antitubercular activity screening

被引:17
|
作者
Sonia, George [1 ]
Ravi, Thengungal Kochupappy [1 ]
机构
[1] Sri Ramakrishna Inst Paramed Sci, Dept Pharmaceut Chem, Coll Pharm, Coimbatore 641044, Tamil Nadu, India
关键词
Pyrrolidine carboxamides; Oxadiazole; Docking; Enoyl-acyl carrier protein (ACP); Reductase inhibitors; Antitubercular activities; ANTIBACTERIAL ACTIVITY; TARGET; TUBERCULOSIS; INHA;
D O I
10.1007/s00044-012-0340-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Pyrrolidine carboxamides have been recognized as potent direct enoyl-acyl carrier protein reductase inhibitors. In our study, the search for new pyrrolidine carboxamides incorporated with various heterocyclic moieties, possessing antitubercular activities is been done. A series of oxadiazolyl pyrrolidine carboxamides (2a-e) were synthesized by reacting pyrrolidine carboxylic acid and oxadiazole amines using HBTU as amide forming agent. The purity of the synthesized compounds was confirmed by physical characterization like melting point and thin layer chromatography. The functional group identification was done based on spectral characterization utilizing, FT-IR, H-1 NMR, C-13 NMR, mass spectral data and elemental analysis. Invitro antitubercular screening was performed by alamar blue assay method on mycobacterium tuberculosis H37Rv.
引用
收藏
页码:3428 / 3433
页数:6
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