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药物化学家的大学教育：八个国家的比较
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今天，偶然翻阅到2000年35卷第1期发表在《European Journal of Medicinal Chemistry（欧洲药物化学杂志）》上的一篇文章，题目是药物化学家的大学教育：八个国家的比较（University education of medicinal chemists: comparison of eight countries）。作者是C.Robin Ganellin、Lester A Mitscher、Bernd Clement、Toshi-Hiko Kobayashi、Emilio Kyburz、 Olivier Lafont、Annie Marcincal、Antonio Monge、Giorgio Tarzia、John G Topliss。文章比较了法国、德国、意大利、日本、西班牙、瑞典、英国和美国等八个国家的药物化学家的大学教育。文章内容还涉及了为攻读药物化学博士学位的学生开设的课程，包括：生物试验、生物化学、组合化学、计算机辅助药物设计、分子模建、定量构效关系、药物分析、药物代谢、酶学、普通实验室技术、分子生物学、NMR分析、有机合成、特殊试剂、专利法规、药物代谢动力学、药理学、物理有机化学、前体药物、放射化学、分离技术、波谱方法、统计学、毒理学。从上面开设的课程数量来看，国外药物化学博士课程的开设时间不会少于1年。所以说药物化学博士攻读四年还是有它的合理性。在作者名单我还看到了John G Topliss的大名，他是“Topliss合成树”的创建者，也是首批使用定量构效关系的科学家之一。
Topliss was part of scientific and man- agement teams that successfully brought a number of drugs to the world market. But one of his most lasting contributions was the development of a more rational, theoretically based approach to analog synthesis than was formerly practiced in the industry. He was one of the first to use quantitative structure-activity relationships (QSARs) methodology, which led him to formulate Operational Schemes for Analog Synthesis in Drug Design (later known as the Topliss Tree) published in 1972, and also the related Manual Hansch Approach, published in 1977. Both are simplified non-mathematical paradigms for rapidly optimizing benzene ring substitution for potency enhancement in a compound series, based on physicochemical principles. The methodology was widely adopted, and is still in use.
https://wap.sciencenet.cn/blog-297341-548930.html
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