Eskitis Institute for Drug Discovery, Griffith University, Don Young Road, Nathan, Queensland 4111, Australia; Queensland Institute of Medical Research, Herston, Queensland 4029, Australia.
Bioorg Med Chem Lett. 2013 Nov 15;23(22):6114-7. doi: 10.1016/j.bmcl.2013.09.015. Epub 2013 Sep 14.
Despite the urgent need for effective antimalarial drugs with novel modes of action no new chemical class of antimalarial drug has been approved for use since 1996. To address this, we have used a rational approach to investigate compounds comprising the primary benzene sulfonamide fragment as a potential new antimalarial chemotype. We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds. Our findings provide a platform to support the further evaluation of primary benzene sulfonamides as a new antimalarial chemotype, including the identification of the target of these compounds in the parasite.
尽管迫切需要具有新型作用模式的有效抗疟药物，但自 1996 年以来，没有新的化学类抗疟药物获得批准使用。为了解决这个问题，我们采用了一种合理的方法来研究包含主要苯磺酰胺片段的化合物，将其作为一种潜在的新型抗疟化学型。我们报告了针对恶性疟原虫敏感（3D7）和耐药（Dd2）寄生虫的十四种主要苯磺酰胺化合物的体外活性。我们的研究结果为进一步评估苯磺酰胺作为新型抗疟化学型提供了一个平台，包括鉴定这些化合物在寄生虫中的靶标。
