抗疟苯甲脒类药物的设计、合成与生物评价。
Reverse-benzamidine antimalarial agents: design, synthesis, and biological evaluation.
机构信息
Institut des Biomolécules Max Mousseron UMR 5247 CNRS-Universités Montpellier I et II, Faculté de Pharmacie, 15 Av Ch Flahault, 34093 Montpellier cedex 5, France.
出版信息
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5815-7. doi: 10.1016/j.bmcl.2010.07.124. Epub 2010 Aug 3.
PMID:20800484
Abstract
In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.
摘要
在双阳离子型胆碱类似物的发展框架内，研究了双-N-烷基脒的 RSA，并设计了一系列新型反苯甲脒衍生物。与亲脂性相反，烷基脒化合物的碱性直接影响其抗疟活性。
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