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新药创制是复杂的智力活动,涉及科学研究、技术创造、产品开发和医疗效果等多维科技活动。每个药物都有自身的研发轨迹,而构建化学结构是最重要的环节,因为它涵盖了药效、药代、安全性和生物药剂学等性质。本栏目以药物化学视角,对有代表性的药物的成功构建,加以剖析和解读。Anacor公司从生化机制出发研究抗菌药,后转向抗真菌药收获了抗甲癣药他伐硼罗;还从炎症的靶标磷酸二酯酶4和炎症因子入手,研发出治疗过敏性皮炎的克立硼罗。研发过程探索了多种可能与渠道,虽然有些与最终目标未能搭界,但始终坚持研究有机硼酸酯类的执着精神,积累了许多经验,终于诞生两个首创药。研发过程涉及的药物化学、分子生物学和作用机制等研究思路,值得借鉴。由于克立硼罗的安全有效和潜在的市场价值,辉瑞公司以52亿美元收购了该公司。本文以药物化学视角简析两个药物的创制过程。
The creation of new drugs is a complex intellectual activity involving multi-dimensional scientific and technological activities such as scientific research, technological creation, product development and medical effects. Each drug has its own development trajectory, and the construction of the chemical structure is the most important part, because it covers the properties such as efficacy, drug substitution, safety and biopharmaceutical. This column from the perspective of medicinal chemistry, representative of the successful construction of drugs, to be analyzed and interpreted. Anacor company from the biochemical mechanism of antimicrobial agents, anti-fungal drugs after the turn of the harvest of anti-onychomycosis Tara boron; also from the target of inflammation phosphodiesterase 4 and inflammatory cytokines, developed to treat atopic dermatitis Kerr Boron. R & D process to explore a variety of possibilities and channels, although some and the ultimate goal of failing to make the junction, but always adhere to the persistence of organic boric esters, has accumulated a lot of experience, and finally the birth of two of the first drugs. R & D process involved in drug chemistry, molecular biology and mechanism of action and other research ideas, it is worth learning from. Pfizer acquired the company for $ 5.2 billion due to its safe and effective market potential. This article analyzes the creation of two drugs from the perspective of medicinal chemistry.