Wernsdorfer W H, Landgraf B, Kilimali V A, Wernsdorfer G
Institute of Specific Prophylaxis and Tropical Medicine, University of Vienna, Austria.
Acta Trop. 1998 Jun 15;70(1):9-15. doi: 10.1016/s0001-706x(97)00141-1.
Benflumetol, a novel antimalarial compound belonging to the fluorenes (2,3-benzindenes), has high blood schizontocidal activity, in vitro and in vivo, against mammalian plasmodia, including chloroquine-resistant Plasmodium falciparum. Due to its molecular structure benflumetol occurs in the dextrorotatory and the laevorotatory form. Normal synthesis yields the racemate of both enantiomers. Enantiomers of some antimalarial drugs possess different specific activity. It was therefore of interest to compare the response of P. falciparum to the enantiomers and the racemate of benflumetol in a variety of fresh, natural isolates. Measuring the concentration-specific inhibition of schizont maturation, the parallel investigation of 29 isolates produced no evidence of substantial activity differences between (+)-benflumetol, (-)-benflumetol and racemic benflumetol, the mean EC-50 values being 8.87, 9.71 and 12.44 nmol/l blood-medium-mixture, respectively.
本芴醇是一种新型抗疟化合物，属于芴类（2,3-苯并茚），在体内外对包括耐氯喹恶性疟原虫在内的哺乳动物疟原虫具有高血内裂殖体杀灭活性。由于其分子结构，本芴醇以右旋和左旋形式存在。常规合成产生两种对映体的外消旋体。一些抗疟药物的对映体具有不同的比活性。因此，比较恶性疟原虫对本芴醇对映体和外消旋体在各种新鲜天然分离株中的反应很有意义。通过测量裂殖体成熟的浓度特异性抑制，对29个分离株的平行研究没有发现（+）-本芴醇、（-）-本芴醇和外消旋本芴醇之间存在实质性活性差异的证据，平均EC-50值分别为8.87、9.71和12.44 nmol/l血-培养基混合物。
