(E)-2-(4-((4-((1-(2,4-二氯苯基)-3-甲基-5-氧-1,5-二氢- 4h -吡唑-4-酰基)甲基)-2-甲氧基苯氧基)甲基)- 1h -1,2,3-三唑-1-基)- n -苯乙酰胺衍生物的合成及抗菌评价

IF 1.1 4区 化学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Cheryl T. Mascarenhas, Jaidip B. Wable, Hemantkumar N. Akolkar, Nirmala R. Darekar, Pradnya J. Prabhu
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引用次数: 0

摘要

目的:目前尚未对(E)-2-(4-((4-(1-(2,4-二氯苯基)-3-甲基-5-氧- 1h -吡唑-4(5H)-乙基)甲基)-2-甲氧基苯氧基)甲基- 1h -1,2,3-三唑-1-基)- n -苯乙酰胺衍生物进行整理。以(E)-1-(2,4-二氯苯基)-4-(3-甲氧基-4-(2-炔-1-基氧基)苄基)-3-甲基- 1h -吡唑-5(4H)- 1 (V)为原料合成(viia - vih)。方法:采用Click化学法合成化合物。我们采用管稀释法检测抗菌和抗真菌活性。结果和讨论:用质谱、1H、13C NMR和IR光谱对8个新合成的化合物进行了验证。对新化合物的抗菌和抗真菌性能进行了测试。7种化合物((VIIa-VIIc), (viie - vih))显示出对一系列细菌菌株的抗菌活性,包括大肠杆菌,铜绿假单胞菌,金黄色葡萄球菌和化脓性链球菌,其活性与药物氨苄西林相当,而(VIIh)与标准药物灰黄霉素相比具有良好的抗白色念珠菌活性。结论: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。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis and Antimicrobial Evaluation of (E)-2-(4-((4-((1-(2,4-Dichlorophenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)methyl)-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide Derivatives

Synthesis and Antimicrobial Evaluation of (E)-2-(4-((4-((1-(2,4-Dichlorophenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)methyl)-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide Derivatives

Objective: There has never been a compilation of (E)-2-(4-((4-((1-(2,4-dichlorophenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)methyl)-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide derivatives produced before. For the synthesis of (VIIa–VIIh), (E)-1-(2,4-dichlorophenyl)-4-(3-methoxy-4-(prop-2-yn-1-yloxy)benzylidene)-3-methyl-1H-pyrazol-5(4H)-one (V) was utilized. Methods: The compounds were synthesized using the Click chemistry process. We used the tube-dilution approach to test for antimicrobial and antifungal activity. Results and Discussion: Mass spectrometry, 1H, 13C NMR, and IR spectroscopy were used to validate the eight newly produced compounds. The antibacterial and antifungal properties of the new compounds were tested. While seven compounds ((VIIa–VIIc), (VIIe–VIIh)) demonstrated antimicrobial activity against a range of bacterial strains, including Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pyogenes, the activity was comparable to that of the drug ampicillin, whereas (VIIh) exhibited good antifungal activity compared to its standard drug Griseofulvin against Candida albicans. Conclusions: We conclude that the newly synthesized 1,2,3-triazoles showed good antibacterial activity and can be used as precursors for drug molecules in the future.

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来源期刊
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry 生物-生化与分子生物学
CiteScore
1.80
自引率
10.00%
发文量
118
审稿时长
3 months
期刊介绍: Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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