Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, Viale A. Doria, 6, 95100, Catania, Italy.
Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, Viale A. Doria, 6, 95100, Catania, Italy.
Eur J Med Chem. 2018 Mar 25;148:410-422. doi: 10.1016/j.ejmech.2018.02.046. Epub 2018 Feb 17.
Benzomorphan, derived by morphine skeleton simplification, has been the subject of exploration in medicinal chemistry for the development of new drugs and pharmacological tools to explore opioid pharmacology in vitro and in vivo. Building upon these evidences, the design and synthesis of benzomorphan-based compounds, appropriately modified at the basic nitrogen and/or the phenolic hydroxyl (8-OH) group, represent a valid and versatile strategy to obtain analgesics. In this review, to improve the body of information in this field, we report structure activity-relationships (SARs) of benzomorphan-based compounds analysing data literature of last 25 years. Collectively, SARs data highlighted that the benzomorphan nucleus represents a template in the achievement of a specific functional profile, by modifying N-substituent or 8-OH group.
苯并吗啡烷通过吗啡骨架简化衍生而来，一直是药物化学领域探索的对象，目的是开发新药和药理学工具，以在体外和体内探索阿片类药物的药理学。在此基础上，对基本氮原子和/或酚羟基（8-OH）基团进行适当修饰的苯并吗啡烷类化合物的设计和合成，代表了获得镇痛药的一种有效且通用的策略。在这篇综述中，为了改进该领域的信息，我们报告了苯并吗啡烷类化合物的构效关系（SAR），分析了过去 25 年的文献数据。总的来说，SAR 数据表明，苯并吗啡烷核是通过修饰 N-取代基或 8-OH 基团来实现特定功能特性的模板。
