苯并三唑介导的新型N-酰基头孢氨苄的合成及其抗菌活性
Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins.
作者信息
Agha Khalid A, Abo-Dya Nader E, Ibrahim Tarek S, Abdel-Aal Eatedal H, Hegazy Wael A
机构信息
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia.
出版信息
Sci Pharm. 2016 Apr 13;84(3):484-496. doi: 10.3390/scipharm84030484.
Cephalexin () was acylated using -acylbenzotriazoles (-) derived from various carboxylic acids including aromatic, heterocyclic and -Pg-α-amino acid to afford -acylcephalexins in excellent yields (82%-96%). Antibacterial screening of the novel cephalosporins revealed that all targets (-) retained the antibacterial activity of cephalexin against (ATCC 6538). -Nicotinylcephalexin () and -(3,4,5-trimethoxybenzoyl)cephalexin () exhibited a broader spectrum of antibacterial activity towards standard strains of (ATCC 6538), (ATCC 842), and (ATCC 10536) as well as a resistant strain of (ATCC 27853).
使用由各种羧酸（包括芳香族、杂环和-Pg-α-氨基酸）衍生而来的α-酰基苯并三唑对头孢氨苄（）进行酰化反应，以优异的产率（82%-96%）得到α-酰基头孢氨苄。对新型头孢菌素的抗菌筛选表明，所有目标产物（）均保留了头孢氨苄对金黄色葡萄球菌（ATCC 6538）的抗菌活性。烟酰基头孢氨苄（）和（3,4,5-三甲氧基苯甲酰基）头孢氨苄（）对金黄色葡萄球菌（ATCC 6538）、大肠杆菌（ATCC 842）和肺炎克雷伯菌（ATCC 10536）的标准菌株以及金黄色葡萄球菌耐药菌株（ATCC 27853）表现出更广泛的抗菌活性。
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