Synthesis and In-Vitro Antimycobacterial Evaluation of 4-Arylidene-2-Phenyl-6-(Aryl)-4,5-Dihydropyridazin-3(2H)-One Derivatives

被引:1
|
作者
Almehmadi, Mazen M. [1 ]
Alsaiari, Ahad Amer [2 ]
Asif, Mohammad [3 ]
机构
[1] Taif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, Taif 21944, Saudi Arabia
[2] Jazan Univ, Coll Appl Med Sci, Dept Med Lab Technol, Jazan, Saudi Arabia
[3] Glocal Univ, Glocal Sch Pharm, Saharanpur 247121, Uttar Pradesh, India
关键词
pyridazinone; antimycobacterial activity; Mycobacterium tuberculosis; synthesis; heterocyclic compounds; drug resistance; spectral data; PYRIDAZINONE DERIVATIVES; ANTITUBERCULAR ACTIVITY; BIOLOGICAL EVALUATION; DESIGN; DRUGS; VASORELAXANT; ANALOGS;
D O I
10.1007/s11094-023-02876-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 4-arylidene-2-phenyl-6-(aryl)-4,5-dihydropyridazin-3(2H)-one derivatives (3a-3g and 3a'-3g') have been synthesized and evaluated as antimycobacterial agents by microplate alamar blue assay (MABA) method. Title compounds 3a-3g and 3a'-3g' were synthesized by reaction of 6-aryl-2-phenyl-4,5-dihydropyridazin-3(2H)-one (2a, 2b) with various aromatic aldehydes. Compounds 2a and 2b were synthesized from 4-aryl-4-oxobutanoic acids (1a,1b) by reaction ofphenyl hydrazine with appropriate aromatic compounds and succinic anhydride. The structures of synthesized compounds have been established by IR, H-1 NMR, and mass spectroscopy and elemental analysis. All synthesized compounds (3a-3g and 3a'-3g') exhibited significant antimycobacterial activity. Compound 3g showed maximum activity and compounds 3b, 3b', 3e, 3e', 3g'showed moderate activity as compared to the reference drugsisoniazid (MIC 3.125 mu g/mL) and streptomycin (MIC 6.25 mu g/mL).
引用
收藏
页码:265 / 273
页数:9
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