Rovnyak G C, Millonig R C, Schwartz J, Shu V
J Med Chem. 1982 Dec;25(12):1482-8. doi: 10.1021/jm00354a018.
A series of novel hexahydrothiopyrano[4,3-c]pyrazoles and related analogues were prepared and tested for antiinflammatory activity by using the mouse active Arthus reaction and the delayed hypersensitivity skin reaction in guinea pigs as primary screens. The compounds of most interest, 18 and 28, were further tested in a model of adjuvant-induced arthritis; in this system, both compounds were active when dosed intraperitoneally but failed to produce significant activity when dosed orally at subtoxic doses.
通过使用小鼠主动Arthus反应和豚鼠迟发型超敏皮肤反应作为初步筛选，制备了一系列新型六氢硫代吡喃并[4,3-c]吡唑及其相关类似物，并测试了它们的抗炎活性。最受关注的化合物18和28，在佐剂诱导的关节炎模型中进行了进一步测试；在该系统中，两种化合物腹腔给药时均有活性，但在亚毒性剂量口服给药时未产生显著活性。
