Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents

被引：9

作者：

Himaja, M. ^{[2
]}

Karigar, Asif ^{[1
]}

Ramana, M. V. ^{[1
]}

Munirajasekhar, D. ^{[2
]}

Sikarwar, Mukesh S. ^{[3
]}

机构：

[1] Maratha Mandals Coll Pharm, Dept Pharmaceut Chem, Belgaum 590016, Karnataka, India

[2] VIT Univ, Sch Adv Sci, Pharmaceut Chem Div, Vellore 632014, Tamil Nadu, India

[3] KLEU Coll Pharm, Dept Pharmacognosy, Belgaum, Karnataka, India

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 06期

关键词：

2-amino-5-aryl-5H-thiazolo[4,3-b]-1,3,4-thiadiazoles; Antitubercular activity; Azetidin-2-ones; Schiff base; MYCOBACTERIUM-TUBERCULOSIS; BIOLOGICAL-ACTIVITY; BETA-LACTAMS; 2-AZETIDINONES; MOIETY;

D O I：

10.2174/157018012800673038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of twelve novel azetedinones 4a-l have been synthesized by cyclocondensation of various Schiff bases of amino thiadiazole with chloroacetyl chloride in the presence of triethylamine. Various novel Schiff bases 3a-l were synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-1, 3,4-thiadiazole with various aryl aldehydes. The synthesized compounds were characterized by FTIR, H-1-NMR, C-13-NMR and mass spectra. The titled compounds 3a-l and 4a-l were evaluated for anti-tubercular activity at a concentration of 0.1-100 mu g/mL by Microplate Blue Alamar Assay method. Azetedinones 4a-l showed very good inhibition against the growth of Mycobacterium tuberculosis compared to compounds 3a-l and standard Streptomycin and Pyrazinamide.

引用

页码：611 / 617

页数：7

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