Defence Research & Development Establishment, Jhansi Road, Gwalior 474002, India.
Eur J Med Chem. 2010 Feb;45(2):430-8. doi: 10.1016/j.ejmech.2009.10.023. Epub 2009 Oct 28.
A series of 1,3,5-trisubstituted pyrazolines were synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive (MRC-02) as well as chloroquine resistant (RKL9) strains of Plasmodium falciparum. The activity was at nano molar concentration. beta-hematin formation inhibition activity (BHIA(50)) of the pyrazolines were determined and correlated with antimalarial activity. A reasonably good correlation (r=0.62) was observed between antimalarial activity (IC(50)) and BHIA(50). This suggests that antimalarial mode of action of this class of compounds appears to be similar to that of chloroquine and involves the inhibition of hemozoin formation. Some of the compounds were showing better antimalarial activity than chloroquine against resistant strain of P. falciparum and were also found active in the in vivo experiment.
一系列 1,3,5-三取代吡唑啉被合成，并对体外抗疟功效进行了评价，针对氯喹敏感（MRC-02）和氯喹耐药（RKL9）的恶性疟原虫株。活性在纳摩尔浓度下。吡唑啉的β-血红素形成抑制活性（BHIA（50））被测定，并与抗疟活性相关联。在抗疟活性（IC（50））和 BHIA（50）之间观察到相当好的相关性（r=0.62）。这表明该类化合物的抗疟作用模式似乎类似于氯喹，涉及血红素形成的抑制。一些化合物在体内实验中显示出比氯喹对耐药株更好的抗疟活性。
