用于抗疟剂的吩恶嗪衍生物的药效学和药代动力学研究。

Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent.

作者信息

Yang Mei, Ge Jian-Feng, Arai Chika, Itoh Isamu, Fu Qiang, Ihara Masataka

机构信息

Research Centre of Medicinal Sciences, Hoshi University, Shinagawa, Tokyo, Japan.

出版信息

Bioorg Med Chem. 2009 Feb 15;17(4):1481-5. doi: 10.1016/j.bmc.2009.01.021. Epub 2009 Jan 15.

DOI:10.1016/j.bmc.2009.01.021

PMID:19181530

Abstract

In vivo antimalarial drug candidates screening test was carried out on a series of water-soluble 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives. Among them, 3-(diethylamino)-7-(piperidin-1-yl)phenoxazin-5-ium chloride (SSJ-206) showing highest efficacy was chosen for further pharmcodynamics and pharmacokinetics study. It was supported from these data that the phenoxazinium salts, SSJ-206, would be one of hopeful candidates as an oral antimalarial drug.

摘要

对一系列水溶性3,7-双（二烷基氨基）吩恶嗪-5-鎓衍生物进行了体内抗疟候选药物筛选试验。其中，选择了显示出最高疗效的3-（二乙氨基）-7-（哌啶-1-基）吩恶嗪-5-鎓氯化物（SSJ-206）进行进一步的药效学和药代动力学研究。这些数据支持吩恶嗪盐SSJ-206有望成为口服抗疟药物的候选药物之一。