3-(4,5-二苯基- 1h -咪唑-2-基)- 1h -吲哚衍生物的合成、抗菌及抑菌活性研究

N. Nirwan, C. Pareek, A. Chohadia, K. Verma
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引用次数: 0

摘要

含吲哚咪唑环的天然和合成化合物已显示出广泛的生物活性。这些吲哚咪唑化合物含有吲哚环和咪唑环。以Amberlyst a- 15为可回收催化剂,在微波照射下,以吲哚-3-甲醛、苯、乙酸铵和取代胺为原料,采用绿色高效的一锅四组分缩合法合成了结构类似于化合物1a-1d和2a-2d的吲哚-咪唑。合成的化合物通过FTIR、1H NMR和质谱进行了结构表征。筛选了这些化合物的抗菌和抗真菌活性,并与标准药物进行了比较。化合物1c是这些化合物中活性最强的衍生物,其最低抑制浓度在09.9 ~ 12.5 μg/mL范围内。化合物1d对白色念珠菌也有较强的抑制作用。化合物对金黄色葡萄球菌、表皮葡萄球菌、大肠杆菌的敏感性依次为1a<1b<1c<1d;对白色念珠菌的敏感性依次为1a<1b<1c<1d。化合物2a对大肠杆菌和白色念珠菌具有良好的抑菌活性。
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Synthesis, Antibacterial, and Antifungal Activities of 3-(4,5-Diphenyl-1H-Imidazol-2-yl)-1H-Indole Derivatives
Indolylimidazole ring-containing natural and synthesized compounds have shown vast biological activities. These indolylimidazole compounds contain both indole and imidazole rings. The indolylimidazole structure resembling compounds 1a-1d and 2a-2d were synthesized by a green and efficient one-pot four components condensation of indole-3-carbaldehyde, benzil, ammonium-acetate, and substituted amines under microwave irradiation using Amberlyst A-15 as a recyclable catalyst. The structures of synthesized compounds were characterized by FTIR, 1H NMR, and Mass spectrometric studies. These compounds' antibacterial and antifungal activities were screened and compared with the standard drug. The compound 1c was found to be the most active derivative in these compounds, with a minimum inhibitory concentration in the range of 09.9 to 12.5 μg/mL. Compound 1d also showed potent activity against Candida albicans. The sensitivity order of compounds was found 1a<1b<1c>1d against Staphylococcus aureus, Staphylococcus epidermidis, and Escherichia coli and 1a<1b<1c<1d for C. albicans. Compound 2a showed good antimicrobial activity against E. coli and C. albicans.
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