Synthesis and Biological Evaluation of Pyrazoline Derivatives Bearing an Indole Moiety as New Antimicrobial Agents

被引：32

作者：

Ozdemir, Ahmet ^{[1
]}

Altintop, Mehlika Dilek ^{[1
]}

Kaplancikli, Zafer Asim ^{[1
]}

Turan-Zitouni, Gulhan ^{[1
]}

Karaca, Hulya ^{[2
]}

Tunali, Yagmur ^{[2
]}

机构：

[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey

[2] Anadolu Univ, Fac Pharm, Dept Pharmaceut Microbiol, TR-26470 Eskisehir, Turkey

来源：

ARCHIV DER PHARMAZIE | 2013年 / 346卷 / 06期

关键词：

Antimicrobial activity; Brine-Shrimp lethality; Chalcone; Indole; Pyrazoline; ANTIFUNGAL AGENTS; ANTIBACTERIAL; INDOLMYCIN; ANTICANCER; RESISTANCE; CHALCONES;

D O I：

10.1002/ardp.201200479

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1-(p-Methylphenyl)-3,5-diaryl-2-pyrazoline derivatives (2a-f) were synthesized via the treatment of 1-(1H-indol-3-yl)-3-aryl-2-propen-1-ones (1a-f) with p-methylphenylhydrazine hydrochloride in hot acetic acid. The structures of these compounds were elucidated by IR, 1H NMR, and mass spectral data and elemental analysis. These compounds were investigated for their antimicrobial activity. Brine-Shrimp lethality assay was carried out to determine the toxicity of the compounds. Compound 2e, which is the pyrazoline derivative bearing the 2,5-dichlorophenyl moiety, can be identified as the most promising agent against Klebsiella pneumoniae (ATCC 13883) and Candida glabrata (ATCC 36583) due to its inhibitory effects on K. pneumoniae and C. glabrata with a MIC value of 100 mu g/mL as a non-toxic agent (LC50>1000 mu g/mL).

引用

页码：463 / 469

页数：7

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