化学通报（印刷版）
化學通報（印刷版）
화학통보（인쇄판）
CHEMISTRY
2009年
11期
973-978
,共6页
桑鹏%邹建卫%许林%黄光东
桑鵬%鄒建衛%許林%黃光東
상붕%추건위%허림%황광동
氟%药物设计%电子效应%立体效应%代谢阻碍%亲脂性
氟%藥物設計%電子效應%立體效應%代謝阻礙%親脂性
불%약물설계%전자효응%입체효응%대사조애%친지성
Fluorine%Drug design%Electronic effect%Steric effect%Metabolic block%Lipophilicity
含氟化合物在近年来上市药物中占据相当比重.药物化学家越来越认识到,在有机化合物中选择性地引入氟原子或含氟基团,可对其生物效应带来微妙的变化.本文从电子效应、代谢阻碍效应、亲脂性效应和立体效应4个方面对氟在药物设计与开发中的应用进行了综述.
含氟化閤物在近年來上市藥物中佔據相噹比重.藥物化學傢越來越認識到,在有機化閤物中選擇性地引入氟原子或含氟基糰,可對其生物效應帶來微妙的變化.本文從電子效應、代謝阻礙效應、親脂性效應和立體效應4箇方麵對氟在藥物設計與開髮中的應用進行瞭綜述.
함불화합물재근년래상시약물중점거상당비중.약물화학가월래월인식도,재유궤화합물중선택성지인입불원자혹함불기단,가대기생물효응대래미묘적변화.본문종전자효응、대사조애효응、친지성효응화입체효응4개방면대불재약물설계여개발중적응용진행료종술.
Fluorine-containing compounds comprise a considerable proportion in recent launched drugs. The medicinal chemists have become more and more conscious that the biological effect of some organic compounds may produce subtle changes through introducing fluorine or fluorinated substituent into their structures. In this paper, the application of fluorination in drug design and development are summarized from the viewpoints of electronic effect, steric effect, metabolic block and lipophilicity.
