Schmidt L H
Antimicrob Agents Chemother. 1985 Feb;27(2):146-50. doi: 10.1128/AAC.27.2.146.
BA-41,799, a tetrahydrofuran derivative that at one time attracted considerable interest as an antimalarial agent because of a combination of structural novelty with activities against infections with Plasmodium berghei and Plasmodium berghei yoelii in mice, has been evaluated for its capacities to effect prophylaxis and radical cure in rhesus monkeys challenged or already infected with sporozoites of the drug-susceptible Ro strain or the pyrimethamine-resistant Ro/PM strain of Plasmodium cynomolgi, and for its capacity to effect suppressive cure of infections with trophozoites of these strains. At doses up to the maximum tolerated, BA-41,799 had only marginal activity against infections with the Ro strain and none against the Ro/PM strain. On the basis of past experiences, the above results suggest that BA-41,799 would have little to offer for prophylaxis, radical cure, or suppression of human infections with Plasmodium vivax.
BA - 41799是一种四氢呋喃衍生物,由于其结构新颖,且对小鼠体内的伯氏疟原虫和约氏疟原虫感染具有活性,一度作为抗疟药物引起了广泛关注。本研究评估了BA - 41799对感染了易感药物的食蟹猴疟原虫Ro株或耐乙胺嘧啶的Ro/PM株子孢子的恒河猴进行预防和根治的能力,以及对这些菌株滋养体感染进行抑制性治疗的能力。在高达最大耐受剂量时,BA - 41799对Ro株感染仅有微弱活性,对Ro/PM株感染则无活性。根据以往经验,上述结果表明BA - 41799对间日疟原虫人类感染的预防、根治或抑制作用不大。