SYNTHESIS, CHARACTERIZATION AND ANTITUBERCULAR ACTIVITY OF 6-(ARYL)-2-(SUBSTITUTED METHYL)-4,5-DIHYDRO(2H)PYRIDAZIN-3-ONE DERIVATIVES AGAINST MYCOBACTERIUM TUBERCULOSIS H37RV

被引:4
|
作者
Asif, Mohammad [1 ]
Abida [2 ]
Imran, Mohd [2 ]
机构
[1] Himalayan Inst Pharm & Res, Dept Pharmaceut Chem, Dehra Dun 248007, Uttarakhand, India
[2] Northern Border Univ, Fac Pharm, Dept Pharmaceut Chem, POB 840, Raffia 91911, Saudi Arabia
来源
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH | 2020年 / 11卷 / 02期
关键词
Pyridazinone; Antitubercular; Mycobacterium; Biological activities; Heterocyclic; synthesis; PYRIDAZINONE DERIVATIVES;
D O I
10.13040/IJPSR.0975-8232.11(2).826-31
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Two series of pyridazinone derivatives. 6-(aryl)-2-(substituted methyl)-4,5-dihydro (2H) pyridazin-3-one derivatives (3a-8a and 3b-8b) were synthesized by reacting 6-phenyl substituted 2,3,4,5-Tetrahydro pyridazin-3-one (2a and 2b) with cyclic secondary amine under Mannich reaction conditions. These final compounds (3a-8a and 3b-8b) were characterized by spectral analysis (IR, (HNMR)-H-1 and mass spectroscopy) and evaluated for anti-tubercular activities against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue assay (MABA) method. Most of the compounds were showed significant anti-tubercular activity. Compounds (7a and 7b) were showed maximum antitubercular activity with 6.25 mu g/ml minimum inhibitory concentration (MIC) value and compounds (4a, 5a, 8a and 3b, 4b, 6b, 8b) were exhibited 12.5 mu g/ml MIC value and other remaining compounds (3a. 6a and 5a) were found less potent (12.5 mu g/ml) MIC value than the reference drugs when compared with reference drugs [pyrizinamide (3.125 mu g/ml)] and (streptomycin 6.25 mu g/ml) MIC values. Among the synthesized pyridazinone derivatives, compound (7a and 7b) emerged as a lead compound with good anti-tubercular activity. These biological activities differences mainly depend on the different type of substitutions on the pyridazinone ring system.
引用
收藏
页码:826 / 831
页数:6
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