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本文报道2-乙酰基-3-苯基-5-对-甲苯磺酰基-7/8H(或甲氧基)-3,3a,4,5-四氢吡唑[4,3-c]喹啉(4)的合成及其药理筛选结果。初步药理筛选表明,化合物19(R~1=R~2=H)、22(R~1=8-OCH_3,R~2=H)以20mg/kg剂量给予雌性大鼠,有避孕作用,低于此剂量则无效。19经结构改造,活性未见提高。有趣的是,7/8-取代或8-甲氧化合物有活性,而相应的7-甲氧类似物无作用,这表明,7-位以不取代为好。若在3-苯基进行取代,则失活。作者前曾报道,无对-甲苯磺酰基的相应的B-环闭联化合物没有抗生育作用。因此,19的骨架似乎是这
It has been reported herein that 2-acetyl-3-phenyl-5-p-toluenesulfonyl-7 / 8H (or methoxy) -3,3a, 4,5-tetrahydropyrazolo [4,3-c] Synthesis and Pharmacological Screening Results of. Preliminary pharmacological screening showed that compounds 19 (R ~ 1 = R ~ 2 = H) and 22 (R ~ 1 = 8-OCH 3, R ~ 2 = H) were administered to female rats at a dose of 20 mg / kg with contraceptive effects and low This dose is invalid. 19 through structural reform, no increase in activity. Interestingly, the 7/8-substituted or 8-methoxy compounds are active, while the corresponding 7-methoxy analogs have no effect, indicating that the 7-position is not substituted as well. If the 3-phenyl substitution, it is inactivated. The authors previously reported that the corresponding B-ring closure without p-toluenesulfonyl has no anti-fertility effect. So, 19’s skeleton seems to be this