Synthesis, Characterization and Antimycobacterial Activity of Some Substituted Phenylpyridazinone Derivatives

被引：5

作者：

Alghamdi, Saad ^{[1
]}

Imran, Mohd ^{[2
]}

Kamal, Mehnaz ^{[3
]}

Asif, Mohammad ^{[4
]}

机构：

[1] Umm Al Qura Univ, Fac Appl Med Sci, Lab Med Dept, Mecca 21955, Saudi Arabia

[2] Northern Border Univ, Fac Pharm, Dept Pharmaceut Chem, POB 840, Rafha 91911, Saudi Arabia

[3] Prince Sattam bin Abdulaziz Univ, Coll Pharm, Dept Pharmaceut Chem, Al Kharj 11942, Saudi Arabia

[4] Glocal Univ, Glocal Sch Pharm, Saharanpur, Uttar Pradesh, India

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2022年 / 55卷 / 12期

关键词：

antitubercular activity; microplate alamar blue assay; Mycobacterium tuberculosis H37Rv; pyridazinone; ANTI-TUBERCULAR ACTIVITY; PYRIDAZINONE DERIVATIVES; ANTICONVULSANT; POTENT; DRUGS;

D O I：

10.1007/s11094-022-02583-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aseries 6-phenyl-2-(substituted methyl)-dihydropyridazinone derivatives (3a-3f) were synthesized using the interaction of 6-phenylpyridazinone with cyclic secondary amine by Mannich reaction and evaluated for antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain by Microplate Alamar Blue Assay (MABA) method. All the synthesized compounds (3a-3f) were characterized by IR, H-1 NMR, and mass spectroscopy methods. The results indicated that 6-phenyl-2-(Imidazol-1-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3b) and 6-phenyl-2-(1,2-dihydro-phenothiazin-10-ylmethyl)-4,5-dihydro-2H-pyridazin-3-one (3f) exhibited highest antimycobacterial activity. Other compounds (3a, 3c-3e) showed less significant antimycobacterial activity. The most effective compounds (3b and 3f) possessed MIC of 6.25 mu g/mL that was equal to that of reference drugs Streptomycin and Ciprofloxacin.

引用

页码：1367 / 1371

页数：5

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