Synthesis and Antimicrobial Evaluation of (E)-1-(2,4-Dichlorophenyl)-4-{3-methoxy-4-[(1-phenyl-1H-1,2,3-triazol-4-yl)methoxy]benzylidene}-3-methyl-1H-pyrazol-5(4H)-one Derivatives

IF 0.9 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
C. T. Mascarenhas, J. B. Wable, H. N. Akolkar, P. J. Prabhu
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引用次数: 0

Abstract

A series of novel pyrazolone-triazole compounds based on (E)-1-(2,4-dichlorophenyl)-4-[3-methoxy-4-(prop-2-yn-1-yloxy)benzylidene]-3-methyl-1H-pyrazol-5(4H)-one was synthesized the click chemistry methodology. Antibacterial and antifungal properties of the new compounds were tested. While seven compounds demonstrated antimicrobial activity against a range of bacterial strains, including Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Streptococcus pyogenes it was comparable to the drug ampicillin whereas one compound exhibited excellent antifungal activity in terms of its standard drug griseofulvin against Candida albicans. Rest of the compounds showed good antifungal activity against Candida albicans when compared to griseofulvin. The newly synthesized 1,2,3-triazoles showed good antibacterial activity and can be used as precursors of drug molecules in the future.

(E)-1-(2,4-二氯苯基)-4-{3-甲氧基-4-[(1-苯基- 1h -1,2,3-三唑-4-基)甲氧基]苄基}-3-甲基- 1h吡唑-5(4H)- 1衍生物的合成及抗菌评价
以(E)-1-(2,4-二氯苯基)-4-[3-甲氧基-4-(pro2 - n-1-yloxy)苄基]-3-甲基- 1h -吡唑-5(4H)- 1为基料合成了一系列新型吡唑酮-三唑化合物。测试了新化合物的抗菌和抗真菌性能。其中7种化合物对大肠杆菌、金黄色葡萄球菌、铜绿假单胞菌和化脓性链球菌等多种细菌具有抗菌活性,与氨苄西林相当,而一种化合物对白色念珠菌的标准药物灰黄霉素具有优异的抗真菌活性。与灰黄霉素相比,其余化合物对白色念珠菌表现出良好的抗真菌活性。新合成的1,2,3-三唑具有良好的抗菌活性,可作为药物分子的前体。
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来源期刊
CiteScore
1.40
自引率
22.20%
发文量
252
审稿时长
2-4 weeks
期刊介绍: Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.
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