Synthesis, In Vitro and In Silico Antibacterial Evaluation of 4,5-Dihydro-1H-Indazoles

被引：2
|
作者：
Khan, Rasool [1 ]
Shah, Faiza [1 ]
Salman, Muhammad [1 ]
Khan, Zahid [1 ]
Tavman, Aydin [2 ]
机构：
[1] Univ Peshawar, Inst Chem Sci, Peshawar 25000, Pakistan
[2] Instanbul Univ, Dept Chem, Istanbul, Turkey
来源：
CHEMISTRYSELECT | 2017年 / 2卷 / 29期
关键词：
4,5-dihydro-1H-indazole; pentane-2,4-dione; 1,5-diaryl; 4-acetyl cyclohexen-3-one; In-vitro anti-bacterial potential; Docking studies; BIOLOGICAL EVALUATION; TRYPANOSOMA-CRUZI; MOLECULAR DOCKING; DRUG DISCOVERY; INDAZOLES; AGENTS; DERIVATIVES; DESIGN; CHALCONES; CONDENSATION;
D O I：
10.1002/slct.201701244
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Synthesis and evaluation of in-vitro and in-silico anti-bacterial potential of a series of 4, 5-dihydro-1H-indazoles is reported here. The synthesis of the target 4,5-dihydro-1H-indazoles was accomplished by reacting 1,5-diaryl,4-acetyl cyclohexen-3-one with hydrazine hydrate and selected hydrazides. All the synthesized compounds were evaluated for their anti-bacterial potential against Escherichia coli, Proteus vulgaris, Staphylococcus aureus and Salmonella typhimurium. Among the synthesized indazoles, N,N-dimethyl-4-(3-methyl-6-phenyl-4,5-dihydro-1H-indazol-4-yl)aniline and 3-methyl-4-(3-nitrophenyl)-1,6-diphenyl-4,5-dihydro-1H-indazole exhibited highest antimicrobial activity against Salmonella typhimurium i.e. MIC50 = 3.85 and 4.12 mg/ml respectively. Docking studies were also carried out to provide an insight into binding interaction with the active site of respective enzyme.
引用
收藏
页码：9364 / 9368
页数：5
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