硝呋替莫的对映体不表现出立体选择性抗克氏锥虫活性、毒性或药代动力学特性。
Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties.
作者信息
Moraes Carolina B, White Karen L, Braillard Stéphanie, Perez Catherine, Goo Junghyun, Gaspar Luis, Shackleford David M, Cordeiro-da-Silva Anabela, Thompson R C Andrew, Freitas-Junior Lucio, Charman Susan A, Chatelain Eric
机构信息
Center for Neglected Diseases Drug Discovery, Institut Pasteur Korea, Bundang-gu, Seongnam-Si, Gyeonggi-do, South Korea.
Centre for Drug Candidate Optimisation, Monash University, Parkville, Victoria, Australia.
出版信息
Antimicrob Agents Chemother. 2015;59(6):3645-7. doi: 10.1128/AAC.05139-14. Epub 2015 Apr 6.
With the aim of improving the available drugs for the treatment of Chagas disease, individual enantiomers of nifurtimox were characterized. The results indicate that the enantiomers are equivalent in their in vitro activity against a panel of Trypanosoma cruzi strains; in vivo efficacy in a murine model of Chagas disease; in vitro toxicity and absorption, distribution, metabolism, and excretion characteristics; and in vivo pharmacokinetic properties. There is unlikely to be any therapeutic benefit of an individual nifurtimox enantiomer over the racemic mixture.
为了改进用于治疗恰加斯病的现有药物，对硝呋莫司的各个对映体进行了特性分析。结果表明，这些对映体在体外对一组克氏锥虫菌株的活性、在恰加斯病小鼠模型中的体内疗效、体外毒性以及吸收、分布、代谢和排泄特性，以及体内药代动力学性质方面均相当。单个硝呋莫司对映体相对于外消旋混合物不太可能有任何治疗益处。
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