新型 3-甲基-1H-吲唑衍生物的合成与抗菌活性评价

Farrukh Shaikh, Muhammad Arif, Mohammad Khushtar, Md Nematullah, Md Azizur Rahman
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引用次数: 2

摘要

本研究旨在合成和评估新型杂环化合物、3-甲基-1H-吲唑衍生物的抗菌活性。研究人员合成了杂环化合物、3-甲基-1H-吲唑衍生物(1a-1d 和 2a-2d),并通过熔点、Rf 值、外观 & 值和溶解度对所有衍生物进行了物理表征,还通过红外光谱和 1H NMR 光谱对其中一些衍生物进行了光谱表征。以环丙沙星为标准药物,采用杯板法评估了所有合成衍生物对革兰氏阳性菌枯草杆菌和革兰氏阴性菌大肠杆菌的抗菌活性。所有合成的杂环化合物、3-甲基-1H-吲唑衍生物(1a-1d 和 2a-2d)都对枯草杆菌和大肠杆菌具有抗菌活性。化合物 1d,即 1-(2-(哌啶-1-基)乙-1-酰基)-3-甲基-1H-吲唑,浓度为 300 微克/毫升,与标准药物环丙沙星相比,对枯草杆菌和大肠杆菌的抗菌活性最佳。合成杂环化合物、3-甲基-1H-吲唑-1-基衍生物的方法既简单又经济,而且合成化合物的收率较高。化合物 1-(2-(哌啶-1-基)乙-1-酰基)-3-甲基-1H-吲唑对枯草杆菌和大肠杆菌的抗菌活性最佳。
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Synthesis and evaluation of antibacterial activity of novel 3-methyl-1H-indazole derivatives

Aim of the study was designed to synthesize and evaluate antibacterial activity of novel heterocyclic compounds, 3-methyl-1H-indazole derivatives. The heterocyclic compounds, 3-methyl-1H-indazole derivatives (1a-1d and 2a-2d) were synthesized; all of them characterized physically by melting point, Rf value, appearance & solubility; and some of them characterized spectroscopically by IR and 1H NMR spectroscopy. All the synthesized derivatives were evaluated for their antibacterial activity against both Gram positive bacteria, Bacillus subtilis and Gram negative bacteria, Escherichia coli by cup plate method using ciprofloxacin as a standard drug. All the synthesized heterocyclic compounds, 3-methyl-1H-indazole derivatives (1a-1d and 2a-2d), had shown antibacterial activity against the B. subtilis and E. coli. Compound 1d i.e., 1-(2-(piperidin-1-yl)ethan-1-oyl)-3-methyl-1H-indazole at the concentration of 300 ​μg/ml showed best antibacterial activity against the bacteria B. subtilis and E. coli as compared to standard drug, ciprofloxacin. The methodology for the synthesis of heterocyclic compounds, 3-methyl-1H-indazol-1-yl derivatives was simple as well as economical and gave better yield of the synthesized compounds. The compound, 1-(2-(piperidin-1-yl)ethan-1-oyl)-3-methyl-1H-indazole had shown best antibacterial activity against the bacteria B. subtilis and E. coli.

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