作为抗真菌剂的高烯丙胺及其相关衍生物的构效关系研究。
Structure-activity relationship study of homoallylamines and related derivatives acting as antifungal agents.
作者信息
Suvire Fernando D, Sortino Maximiliano, Kouznetsov Vladimir V, Vargas M Leonor Y, Zacchino Susana A, Cruz Uriel Mora, Enriz Ricardo D
机构信息
Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis (U.N.S.L.), Chacabuco 917, 5700 San Luis, Argentina.
出版信息
Bioorg Med Chem. 2006 Mar 15;14(6):1851-62. doi: 10.1016/j.bmc.2005.10.036. Epub 2005 Nov 10.
The synthesis, in vitro evaluation, and structure-activity relationship studies of homoallylamines and related derivatives acting as antifungal agents are reported. Among them, compounds N-(4-bromophenyl)-N-(2-furylmethyl)amine and N-(4-chlorophenyl)-N-(2-furylmethyl)amine reported here exhibited remarkable antifungal activity against dermatophytes. Theoretical calculations allow us to determine the minimal structural requirements to produce the antifungal response and can provide a guide for the design of compounds with these properties.
本文报道了作为抗真菌剂的高烯丙胺及其相关衍生物的合成、体外评价以及构效关系研究。其中，本文报道的化合物N-(4-溴苯基)-N-(2-呋喃基甲基)胺和N-(4-氯苯基)-N-(2-呋喃基甲基)胺对皮肤癣菌表现出显著的抗真菌活性。理论计算使我们能够确定产生抗真菌反应的最小结构要求，并可为设计具有这些特性的化合物提供指导。
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