Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins

被引：33

作者：

Agha, Khalid A. ^{[1
]}

Abo-Dya, Nader E. ^{[1
,2
]}

Ibrahim, Tarek S. ^{[1
]}

Abdel-Aal, Eatedal H. ^{[1
]}

Hegazy, Wael A. ^{[3
]}

机构：

[1] Zagazig Univ, Dept Organ Pharmaceut Chem, Fac Pharm, Zagazig 44519, Egypt

[2] Univ Tabuk, Dept Pharmaceut Chem, Fac Pharm, Tabuk 71491, Saudi Arabia

[3] Zagazig Univ, Dept Microbiol & Immunol, Fac Pharm, Zagazig 44519, Egypt

来源：

SCIENTIA PHARMACEUTICA | 2016年 / 84卷 / 03期

关键词：

acylation; antibiotics; benzotriazolides; drug research;

D O I：

10.3390/scipharm84030484

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Cephalexin (1) was acylated using N-acylbenzotriazoles (3a-k ') derived from various carboxylic acids including aromatic, heterocyclic and N-Pg-alpha-amino acid to afford N-acylcephalexins in excellent yields (82%-96%). Antibacterial screening of the novel cephalosporins revealed that all targets (4a-j) retained the antibacterial activity of cephalexin against Staphylococcus aureus (ATCC 6538). N-Nicotinylcephalexin (4c) and N-(3,4,5-trimethoxybenzoyl) cephalexin (4g) exhibited a broader spectrum of antibacterial activity towards standard strains of Staphylococcus aureus (ATCC 6538), Paenibacillus polymyxa (ATCC 842), and Escherichia coli (ATCC 10536) as well as a resistant strain of Pseudomonas aeruginosa (ATCC 27853).

引用

页码：484 / 496

页数：13

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