苯基取代苄胺类抗真菌剂的合成及其构效关系：一种用于全身治疗的新型苄基苄胺类抗真菌剂。
Synthesis and structure-activity relationships of phenyl-substituted benzylamine antimycotics: a novel benzylbenzylamine antifungal agent for systemic treatment.
作者信息
Nussbaumer P, Dorfstätter G, Grassberger M A, Leitner I, Meingassner J G, Thirring K, Stütz A
机构信息
Department of Dermatology, SANDOZ Forschungsinstitut, Vienna, Austria.
出版信息
J Med Chem. 1993 Jul 23;36(15):2115-20. doi: 10.1021/jm00067a010.
Derivatives of the benzylamine antimycotics with an extra phenyl ring incorporated in the side chain have been prepared and their antifungal activity evaluated. The potency is strongly dependent on the distance between the two phenyl groups and the type of spacer. Linking the aryl rings with a quaternary carbon atom resulted in the identification of highly active compounds 7f and 12a, having a novel 4-benzylbenzylamine side chain. Compound 7f and its 7-benzo[b]thienyl analogue 12a show significantly enhanced efficacy, in particular against Candida albicans, and are among the most potent allyl/benzylamine antimycotics identified so far. Extended investigations with the benzylbenzylamine derivative 7f revealed that, in addition to the enhanced antimycotic profile, the compound is the first representative of the benzylamine antimycotics suitable for systemic treatment.
已制备了侧链中并入额外苯环的苄胺抗真菌剂衍生物，并对其抗真菌活性进行了评估。效力强烈依赖于两个苯基之间的距离以及间隔基团的类型。将芳环与季碳原子相连导致鉴定出具有新型4-苄基苄胺侧链的高活性化合物7f和12a。化合物7f及其7-苯并[b]噻吩基类似物12a显示出显著增强的效力，尤其是对白色念珠菌，并且是迄今为止鉴定出的最有效的烯丙基/苄胺抗真菌剂之一。对苄基苄胺衍生物7f的进一步研究表明，除了增强的抗真菌谱外，该化合物是适合全身治疗的苄胺抗真菌剂的首个代表。
Zotero 插件