先导化合物的优化与候选药物的确定要点.pptVIP

由研究向开发的过渡 对12个体外活性与阳性对照药塞来昔布相当(在1个数量级内)的化合物进一步做体内筛选试验 * compound No dose mg/kg Number of rats Volume of edema after inflammation and percentage of inhibition (%) 2 hr 3 hr 4 hr control vehicle 8 45.8±12.9 61.2±11.6 60.2±14.5 Bap-801 10 8 44.1±6.4 46.2±13.7 (24.5) 48.6±16.5 (19.3) Bap-802 10 8 31.0±17.9 37.2±9.6 (39.2) 31.2±10.7 (48.2) Bap-805 10 8 38.8±9.8 38.9±11.9 (36.4) 34.0±12.4 (43.5) Bap-807 10 8 40.8±8.8 45.4±19.4 (25.8) 38.1±12.4 (36.7) Bap-902 10 8 46.4±7.0 47.2±13.3 (22.8) 43.8±14.5 (27.2) Bap-904 10 8 22.9±5.9 31.7±13.9 (48.2)