Synthesis and Antimicrobial Activity of New Isoxazolyl Benzo[1,4] diazepine-5-one Derivatives

被引:5
|
作者
Ponduri, Rajasekhar [1 ,2 ]
Kumar, Pramod [1 ]
Vadali, Lakshmana Rao [2 ]
机构
[1] IST, CCST, JNTU H Coll Engn, Hyderabad 500085, Telangana, India
[2] Mylan Labs Ltd, Hyderabad, Telangana, India
来源
CHEMISTRYSELECT | 2018年 / 3卷 / 35期
关键词
Antimicrobial activity; Fe-AcOH; Isoxazolyl benzodiazepine-5-ones; Reductive cyclization; MICROWAVE-ASSISTED SYNTHESIS; ANTICANCER ACTIVITY; IN-VITRO; BIOLOGICAL EVALUATION; 1,5-BENZODIAZEPINES; EFFICIENT; INDOLYL; ANALOGS; DESIGN; POTENT;
D O I
10.1002/slct.201802371
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of novel isoxazolyl-1,4-benzodiazepine-5-ones 4 have been synthesized by the reaction of phenacyl isoxazolylamines 1 with o-nitrobenzoic acids 2 to furnish different (E)-N-(3-methyl-5-styrylisoxazol-4-yl)-2-nitro-N-(2-oxo-2-phenylethyl)benzamides 3, which on treatment with Fe-AcOH underwent reductive cyclization to afford the target compounds 4a-w. The newly synthesized compounds were characterized by IR, (HNMR)-H-1, (CNMR)-C-13, and HRMS analysis. The target compounds 4a-w were evaluated for their invitro antimicrobial activity. Among the synthesized compounds, compounds 4r, 4s, 4t, 4u, 4v and 4w showed potent antimicrobial activity as compared with the reference drugs. Most of the newly synthesized title compounds have shown good to excellent antimicrobial activity.
引用
收藏
页码:10108 / 10112
页数:5
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