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(4,5-二芳基-4H-1,2,4-三唑-3-基)甲基丙烯酸衍生物的抗菌及中枢神经系统活性

ANTIBACTERIAL AND CENTRAL NERVOUS SYSTEM ACTIVITY OF (4,5-DIARYL-4H-1,2,4-TRIAZOL-3-YL)METHACRYLIC ACID DERIVATIVES.

作者信息

Paprocka Renata, Modzelewska-Banachiewicz Bozena, Kutkowska Jolanta, Pawlowskp Kamil, Piatkowska-Chmieiv Iwona, Jagiello-Wojtowicz Ewa

出版信息

Acta Pol Pharm. 2017 Jan;74(1):289-292.

Abstract

The series of 1,2,4-triazole derivatives containing methacrylic acid moiety were synthesized in reaction of N3-substituted amidrazones with itaconic anhydride. Preliminary calculated bioavailability parameters of obtained compounds suggested good penetration via cell membranes and their good absorption after oral intake. Antimicrobial evaluation in vitio showed diverse activity of obtained triazoles mainly on Gram-positive bacterial strains. One derivative was also examined to determine the effect on the central nervous system of mice.

摘要

通过N3-取代的脒腙与衣康酸酐反应合成了一系列含有甲基丙烯酸部分的1,2,4-三唑衍生物。所得化合物初步计算的生物利用度参数表明其具有良好的细胞膜穿透性以及口服后的良好吸收性。体外抗菌评估显示,所得三唑类化合物主要对革兰氏阳性菌菌株具有多样的活性。还对一种衍生物进行了检测,以确定其对小鼠中枢神经系统的影响。

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