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Synthesis, In Vitro and In Silico Antibacterial Evaluation of 4,5‐Dihydro‐1 H ‐Indazoles
Author(s) -
Khan Rasool,
Shah Faiza,
Salman Muhammad,
Khan Zahid,
Tavman Aydin
Publication year - 2017
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201701244
Subject(s) - proteus vulgaris , chemistry , antimicrobial , in silico , escherichia coli , salmonella , indazole , in vitro , docking (animal) , aniline , enzyme , staphylococcus aureus , stereochemistry , proteus , combinatorial chemistry , nuclear chemistry , biochemistry , bacteria , organic chemistry , biology , gene , medicine , genetics , nursing
Synthesis and evaluation of in‐vitro and in‐silico anti‐bacterial potential of a series of 4, 5‐dihydro‐1 H ‐indazoles is reported here. The synthesis of the target 4,5‐dihydro‐1 H‐ 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‐1 H ‐indazol‐4‐yl)aniline and 3‐methyl‐4‐(3‐nitrophenyl)‐1,6‐diphenyl‐4,5‐dihydro‐1 H ‐indazole exhibited highest antimicrobial activity against Salmonella typhimurium i. e. MIC 50 = 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.