ELQ-300 是一种有效、有口服生物活性的抗疟疾剂,结合并抑制细胞色素 bc1 复合物 (cyt bc1) 的还原 (Qi) 位点。
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ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1)[1]. ELQ-300 sensitizes P. falciparum Dd2, Tm90-C2B, and D1 strains with IC50s of 6.6, 4.6 and 160 nM, respectively[1].
[1]. Stickles AM, et al. Subtle changes in endochin-like quinolone structure alter the site of inhibition within the cytochrome bc1 complex of Plasmodium falciparum. Antimicrob Agents Chemother. 2015 Apr;59(4):1977-82.
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