CsF-Celite catalyzed facile N-alkylation of 2(3H)-benzoxazolones and antimicrobial properties of 2-substituted benzoxazole and 3-substituted-2(3H)-benzoxazolone derivatives

被引：17
|
作者：
Murty, M. S. R. [1 ]
Ram, Kesur R. [1 ]
Rao, Rayudu Venkateswara [1 ]
Yadav, J. S. [1 ]
Murty, U. S. N. [2 ]
Kumar, K. Pranay [2 ]
机构：
[1] Indian Inst Chem Technol, Discovery Lab, Organ Chem Div 1, Hyderabad 500607, Andhra Pradesh, India
[2] Indian Inst Chem Technol, Div Biol, Hyderabad 500607, Andhra Pradesh, India
来源：
MEDICINAL CHEMISTRY RESEARCH | 2011年 / 20卷 / 05期
关键词：
Benzoxazole; Benzoxazolone; Cyclic amine; Cesium fluoride-Celite; Antibacterial and antifungal; ANTIINFLAMMATORY ACTIVITY; ANTICANCER; ANALOGS; ACID; HETEROCYCLES; ETHERS; ESTERS;
D O I：
10.1007/s00044-010-9367-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and antimicrobial activity studies of a new series of cyclic amine containing benzoxazoles and benzoxazolone-2(3H)-ones derivatives were described. The alkylation of benzoxazolone was carried out using cesium fluoride-Celite. The newly synthesized compounds with the influence of the induction of the cyclic amine moiety in the benzoxazole scaffold have been evaluated with respect to the antibacterial and antifungal activity. The 2-cyclic amine-1,3-benzoxazoles (5a-l), 5-chloro-3-alkyl substituted-1,3-benzoxazol-2(3H)-ones (8a-f), and 3-[3-(cyclic amine)propyl]-1,3-benzoxazol-2(3H)-ones (9a-f) were synthesized. These derivatives were tested for antibacterial and antifungal activity. Among the compounds tested, 8c and 9f showed moderate to good antibacterial and antifungal activity. Compound 8a showed good antifungal activity.
引用
收藏
页码：626 / 636
页数：11
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