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Synthesis and Antibacterial Evaluation of (E)-5-Arylidene-6-Methyl-4,5-Dihydropyridazin-3(2)-Thione Derivatives
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2022-01-13 , DOI: 10.1007/s11094-021-02515-9
Saad Alghamdi 1 , Mohd. Imran 2 , Mehnaz Kamal 3 , Mohammad Asif 4
Affiliation  

Some(E)-5-arylidene-6-methyl-4,5-dihydropyridazin-3(2H)-thione derivatives (5a-5f) were synthesized and evaluated as antimicrobial agents against Gram positive bacteria Staphylococcus aureus, Bacillus subtilis, and Gram negative bacteria Escherichia coli, and Pseudomonas aeruginosa strains. All the title compounds were characterized by their physical (TLC and M. P.), spectral (IR, 1H NMR) and mass spectroscopy (MS) data. Test results show that compounds 5b and 5e were found to be most effective antibacterial agents against both Gram positive and Gram negative bacterial strains. The presence of an electron attractor group on the aromatic ring as chloro group (5b) is favorable for that antibacterial activity. Derivatives (5c, 5d, 5f) containing the aromatic ring substituted by an electron donor groups (-OCH3, OH) inhibit the activity. All the newly synthesized compounds exhibit promising antimicrobial properties.



中文翻译:

(E)-5-Arylidene-6-Methyl-4,5-Dihydropyridazin-3(2)-Thione 衍生物的合成及抗菌评价

合成了一些 (E)-5-arylidene-6-methyl-4,5-dihydropyridazin-3(2H)-thione 衍生物 (5a-5f) 作为抗革兰氏阳性细菌金黄色葡萄球菌枯草芽孢杆菌和革兰氏菌的抗菌剂阴性菌大肠杆菌铜绿假单胞菌菌株。所有标题化合物均通过其物理(TLC 和 MP)、光谱(IR,1H NMR)和质谱(MS)数据。测试结果表明,化合物 5b 和 5e 被发现是对革兰氏阳性和革兰氏阴性细菌菌株最有效的抗菌剂。芳环上作为氯基团(5b)的电子吸引基团的存在有利于该抗菌活性。含有被电子供体基团(-OCH 3 , OH)取代的芳环的衍生物(5c、5d、5f)抑制活性。所有新合成的化合物都具有良好的抗菌性能。

更新日期:2022-01-13
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