Instituto de Investigaciones Fármaco Bioquímicas, Facultad de Ciencias Farmacéuticas y Bioquímicas, Universidad Mayor de San Andrés, Avenida Saavedra 2224, Miraflores, La Paz, Bolivia.
Exp Parasitol. 2013 Oct;135(2):456-8. doi: 10.1016/j.exppara.2013.08.008. Epub 2013 Aug 25.
A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC₅₀ ≤ 1 μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.
评估了一系列对特权菲咯啉骨架进行结构修饰的衍生物对氯喹敏感的恶性疟原虫 F32 菌株的抗疟活性。两种化合物对疟原虫表现出相当大的抑制作用(IC₅₀ ≤ 1 μg/mL),其中一种在抗氯喹菌株中保持相同的活性。这是该类型支架抗疟活性的第一个记录,为抗疟活性提供了一个新的结构基序作为新的先导。