药代动力学在新药研发中的作用参考幻灯片.pptVIP

N O N N O S O O O N O N H F F F O O N O N N O S O O O O O N H F F F O O N O N N O S O O O O O N H F F F O O pKa = 10 pKa = 8.4 pKa = 6.5 P reduced %= 0% P reduced %= 7% P reduced %= 12% SAR: pKa vs. permeability 实例：结构优化和吸收率分析 31 N O N N O O O N S N N N H F F F O O N O N N O S O O O N S N N N H H Chiral F F F O O N O N N O O O N S N N F F F O O N O N N O S O O O N S N N + F F F O O SAR: permeability vs. efficacy 实例：结构优化和吸收率和活性的分析 IC 50 = 2 uM P reduced %= 0% IC 50 = 0.012 uM P reduced %= 0% IC 50 = 1.1 uM P reduced %= 17% IC 50 = 0.025 uM P reduced %= 15% 32 小结：体外和离体药物吸收实验系统 体外人大肠癌细胞模型 (in