Microwave‐assisted döbner synthesis of 2‐phenylquinoline‐4‐carboxylic acids and their antiparasitic activities
作者:Gisela C. Muscia、Juan P. Carnevale、Mariela Bollini、Silvia E. Asís
DOI:10.1002/jhet.5570450251
日期:2008.3
A series of twelve substituted 2-phenylquinoline-4-carboxylic acids analogous to antimalarial and antileishmanial natural products was developed via the Döbner reaction employing microwave irradiation (MW). The products were obtained in moderate yields in 0.5-3 minutes and nine of them were evaluated in vitro against the parasites responsible for malaria, leishmaniasis and trypanosomiasis diseases
通过利用微波辐射(MW)的Döbner反应,开发了一系列类似于抗疟和抗疟疾天然产物的十二种取代的2-苯基喹啉-4-羧酸。在0.5至3分钟内以中等产量获得了该产品,并在体外对其中9种产品进行了抗疟疾,利什曼病和锥虫病的寄生虫评估(世界卫生组织,瑞士)。四种化合物分别对克氏锥虫具有活性,另外两种化合物分别对恶性疟原虫和婴儿利什曼原虫具有活性。