Synthesis and Antiplasmodial and Antimycobacterial Evaluation of New Nitroimidazole and Nitroimidazooxazine Derivatives
作者:Matshawandile Tukulula、Rajni-Kant Sharma、Maïa Meurillon、Aman Mahajan、Krupa Naran、Digby Warner、Jianxing Huang、Belew Mekonnen、Kelly Chibale
DOI:10.1021/ml300362a
日期:2013.1.10
The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b, exhibited potent activity against the chloroquine-resistant K1 strain of Plasmodium falciparum. Furthermore, a notable number from the tetrazole series were significantly more active
描述了两个新系列的硝基咪唑和硝基咪唑并恶嗪衍生物的合成和抗疟原虫和抗分枝杆菌的评价。这些化合物中的大多数,尤其是杂交体9d、9f和14b,对恶性疟原虫的氯喹抗性 K1 菌株表现出有效的活性。此外,来自四唑系列的显着数字对结核分枝杆菌的活性明显高于标准结核病药物卡那霉素。