新型1,2,4-恶二唑类肽模拟物的合成、抗炎及抗菌活性

Synthesis, anti-inflammatory and antimicrobial activities of new 1,2,4-oxadiazoles peptidomimetics.

作者信息

Leite A C, Vieira R F, de Wanderley A G, Afiatpour P, Ximenes E C, Srivastava R M, de Oliveira C F, Medeiros M V, Antunes E, Brondani D J

机构信息

Departamento de Ciencias Farmacêuticas, Cidade Universitária, Universidade Federal de Pernambuco, Recife-PE, Brazil.

出版信息

Farmaco. 2000 Nov-Dec;55(11-12):719-24. doi: 10.1016/s0014-827x(00)00099-9.

DOI:10.1016/s0014-827x(00)00099-9

PMID:11204948

Abstract

A new series of 1,2,4-oxadizoles 6a-g have been synthesised in good yields using the peptide synthesis strategy. The prepared compounds were tested for anti-inflammatory and antimicrobial activities. The anti-inflammatory activities were determined in the rat paw oedema induced by carrageenin. Compounds 6a, c, f and g (i.v.) significantly inhibited the rat paw oedema induced by carrageenin depending upon the dose employed. The compounds were also evaluated for their in vitro antimicrobial activity. Some compounds were found to have significant activity against Gram positive and Gram negative microorganisms.

摘要

采用肽合成策略，以良好的产率合成了一系列新的1,2,4-恶二唑6a - g。对所制备的化合物进行了抗炎和抗菌活性测试。在角叉菜胶诱导的大鼠足爪水肿模型中测定其抗炎活性。化合物6a、c、f和g（静脉注射）根据所用剂量，显著抑制了角叉菜胶诱导的大鼠足爪水肿。还评估了这些化合物的体外抗菌活性。发现一些化合物对革兰氏阳性和革兰氏阴性微生物具有显著活性。