Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols
Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols
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DOI：
10.1016/j.bmc.2006.10.006
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发表时间：
2007-01-01
影响因子：
3.5
通讯作者：
Singh, Inder Pal
中科院分区：
文献类型：
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作者：
Bharate, Sandip B.;Khan, Shabana I.;Singh, Inder Pal
在本文中，我们研究了几种新合成的O-烷基化间苯三酚化合物（11-19）的抗利什曼原虫、抗疟疾、抗菌和抗真菌活性，这些化合物是天然存在的抗疟疾化合物1的类似物。类似物12和16对杜氏利什曼原虫前鞭毛体具有抗利什曼原虫活性，IC（50）分别为5.3和4.2 μ g/mL。天然存在的单体甲酰化酰基间苯三酚化合物，grandinol（2），jensenone（3），和它们的类似物（29-37），也被合成和评价抗利什曼原虫，抗疟疾，抗菌，和抗真菌活性。其中，grandinol和jensenone表现出轻度至中度的抗菌，抗真菌，抗利什曼原虫的活动。Jensenone（3）对白色念珠菌有效，IC 50为5.5 μ g/mL，但对新型隐球菌和耐甲氧西林金黄色葡萄球菌无效。其中，34对白色念珠菌和念珠菌的活性最强。对新生念珠菌的IC（50）分别为2.0和2.5 μ g/mL，对白色念珠菌具有杀真菌作用。(c)2006爱思唯尔有限公司保留所有权利。
In the present article, we examined the antileishmanial, antimalarial, antibacterial, and antifungal activities of several newly synthesized O-alkylated phloroglucinol compounds (11-19) which are analogues of the naturally occurring antimalarial compound 1. Analogues 12 and 16 exhibited antileishmanial activity against, Leishmania donovani promastigotes with IC(50)s of 5.3 and 4.2 mu g/mL, respectively. Naturally occurring monomeric formylated acylphloroglucinol compounds, grandinol (2), jensenone (3), and their analogues (29-37), were also synthesized and evaluated for antileishmanial, antimalarial, antibacterial, and antifungal activities. Amongst these, both grandinol and jensenone showed mild to moderate antibacterial, antifungal, and antileishmanial activities. Jensenone (3) was effective against Candida albicans with an IC50 of 5.5 mu g/mL but was ineffective against Cryptococcus neoformans and methicillin-resistant Staphylococcus aureus. Among the analogues, 34 was the most active against C albicans and C. neoformans with IC(50)s of 2.0 and 2.5 mu g/mL, respectively, and was fungicidal toward Candida albicans. (c) 2006 Elsevier Ltd. All rights reserved.