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先导化合物结构优化策略（一）——改变代谢途径提高代谢稳定性
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TLDR
本文主要综述了通过改变代谢途径提高代 谢稳定性的先导化合物结构优化策略.Abstract:
先导化合物结构优化是新药研发的关键环节。通过改变先导化合物的代谢途径可以改善化合物的药代动力学特性, 延长药物在体内的作用时间, 增强代谢稳定性, 提高生物利用度。本文主要综述了通过改变代谢途径提高代谢稳定性的先导化合物结构优化策略, 包括封闭代谢位点、降低脂溶性、骨架修饰、生物电子等排以及前药等。read more
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Can the pharmaceutical industry reduce attrition rates
Ismail Kola,John Landis +1 more
TL;DR: The pharmaceutical industry faces considerable challenges, both politically and fiscally, and the fiscal pressures that face the industry from the perspective of R&D are dealt with.
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Cytochrome P-450 Polymorphisms and Response to Clopidogrel
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Synopsis of some recent tactical application of bioisosteres in drug design.
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Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
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