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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.
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页码:9364 / 9368
页数:5
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