V2EX bioisosterism

Bioisosterism

Definition|释义

生物等排体替换(bioisosterism):药物化学中的一种设计思路,指用在大小、形状、电子性质等方面相似的原子或基团去替换分子中的某部分,以期在尽量保持原有生物活性的同时,改善性质(如稳定性、溶解度、选择性、代谢、毒性等)。该词也常用于更广义的“结构替换以优化药效与药代”的讨论。(相关概念还包括 isosterismbioisostere。)

Pronunciation (IPA)|发音(IPA)

/ba.o.a.s.str.zm/

Examples|例句

A fluorine substitution is a common strategy in bioisosterism.
用氟原子进行替换是生物等排体替换中的常见策略。

Through bioisosterism, the team replaced an amide with a bioisostere to improve metabolic stability without losing potency.
通过生物等排体替换,团队用一种生物等排体取代酰胺基团,在不降低效力的情况下提高了代谢稳定性。

Etymology|词源

bio- 意为“生命、生物”,isoster- 源自希腊语词根,含义与“等(iso-)+ 体积/占位(stere-,与 stereos ‘固体、立体’相关)”的概念相连,**-ism** 表示“说/现象/方法”。整体字面可理解为“与生物作用相关的等占位(等排体)替换方法”。该概念在20世纪中期的药物化学发展中被系统化,用于把“结构相似”与“作用相近/性质可调”联系起来。

Related Words|相关词汇

In Literature|文学与著作中的用例

  • Friedman, H. L. (1951) Influence of isosteric replacements upon biological activity(经典论文之一,常被视为将“bioisosterism/生物等排体”思想引入药物设计讨论的重要早期文献)
  • Burger’s Medicinal Chemistry and Drug Discovery(《伯格药物化学与药物发现》;在结构修饰与先导优化章节中常讨论 bioisosterism)
  • The Practice of Medicinal Chemistry(《药物化学实践》;在先导化合物优化、官能团替换策略中出现)
  • Foye’s Principles of Medicinal Chemistry(《福伊药物化学原理》;在SAR与结构改造策略中出现)
About     Help     Advertise     Blog     API     FAQ     Solana     3700 Online   Highest 6679       Select Language
创意工作者们的社区
World is powered by solitude
VERSION: 3.9.8.5 38ms UTC 05:02 PVG 13:02 LAX 22:02 JFK 01:02
Do have faith in what you're doing.
ubao msn snddm index pchome yahoo rakuten mypaper meadowduck bidyahoo youbao zxmzxm asda bnvcg cvbfg dfscv mmhjk xxddc yybgb zznbn ccubao uaitu acv GXCV ET GDG YH FG BCVB FJFH CBRE CBC GDG ET54 WRWR RWER WREW WRWER RWER SDG EW SF DSFSF fbbs ubao fhd dfg ewr dg df ewwr ewwr et ruyut utut dfg fgd gdfgt etg dfgt dfgd ert4 gd fgg wr 235 wer3 we vsdf sdf gdf ert xcv sdf rwer hfd dfg cvb rwf afb dfh jgh bmn lgh rty gfds cxv xcv xcs vdas fdf fgd cv sdf tert sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf sdf shasha9178 shasha9178 shasha9178 shasha9178 shasha9178 liflif2 liflif2 liflif2 liflif2 liflif2 liblib3 liblib3 liblib3 liblib3 liblib3 zhazha444 zhazha444 zhazha444 zhazha444 zhazha444 dende5 dende denden denden2 denden21 fenfen9 fenf619 fen619 fenfe9 fe619 sdf sdf sdf sdf sdf zhazh90 zhazh0 zhaa50 zha90 zh590 zho zhoz zhozh zhozho zhozho2 lislis lls95 lili95 lils5 liss9 sdf0ty987 sdft876 sdft9876 sdf09876 sd0t9876 sdf0ty98 sdf0976 sdf0ty986 sdf0ty96 sdf0t76 sdf0876 df0ty98 sf0t876 sd0ty76 sdy76 sdf76 sdf0t76 sdf0ty9 sdf0ty98 sdf0ty987 sdf0ty98 sdf6676 sdf876 sd876 sd876 sdf6 sdf6 sdf9876 sdf0t sdf06 sdf0ty9776 sdf0ty9776 sdf0ty76 sdf8876 sdf0t sd6 sdf06 s688876 sd688 sdf86