一些 2,3-二取代的 3H-喹唑啉-4-酮的合成及抗利什曼原虫和抗菌活性。

Synthesis and antileishmanial and antimicrobial activities of some 2,3-disubstituted 3H-quinazolin-4-ones.

机构信息

Institute of Chemical Sciences, University of Peshawar, Peshawar, Pakistan.

出版信息

J Enzyme Inhib Med Chem. 2010 Aug;25(4):451-8. doi: 10.3109/14756360903309412.

PMID:20235747

Abstract

A series of 2,3-disubstituted 3H-quinazolin-4-ones was synthesized. Antimicrobial activities of the synthesized compounds were investigated against Gram (+ve) and Gram (-ve) bacteria, including B. subtilis, S. aureus, S. flexneri, P. aeruginosa, and S. typhi, and six fungi, namely Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glabrata using the broth microdilution method. Compounds 9, 11, and 12 showed significant activities against the selected bacterial cultures, while 7-10, 12, 15, and 16 showed good to moderate antifungal activities. Compound 11 exhibited strongest leishmanicidal activity against Leishmania major (MHOM/PK/88/DESTO) promastigotes, while other compounds showed weak to moderate leishmanicidal activities.

摘要

合成了一系列 2,3-二取代的 3H-喹唑啉-4-酮。采用肉汤微量稀释法，对合成的化合物进行了抗革兰氏阳性（+ve）和革兰氏阴性（-ve）细菌（包括枯草芽孢杆菌、金黄色葡萄球菌、福氏志贺菌、铜绿假单胞菌和伤寒沙门氏菌）和六种真菌（包括长须毛癣菌、白色念珠菌、黄曲霉、犬小孢子菌、茄病镰刀菌和光滑念珠菌）的抗菌活性研究。化合物 9、11 和 12 对所选的细菌培养物表现出显著的活性，而 7-10、12、15 和 16 表现出良好到中等的抗真菌活性。化合物 11 对利什曼原虫（MHOM/PK/88/DESTO）前鞭毛体表现出最强的杀利什曼原虫活性，而其他化合物则表现出弱到中等的杀利什曼原虫活性。