Bernard M, Bober M, Krzysztofik B, Skoczna J, Stochla K, Szymczak-Meyer L, Westfal I, Wrzeciono U
Pharmazie. 1984 Jul;39(7):464-6.
Morpholids, N-methylpiperazids, piperidids and pyrrolidids of 5-methyl, 3,5-dimethyl-1-phenyl-4-pyrazolthioacetic acid and 3,5-dimethyl-1-phenyl-4-pyrazolcarbonic acid 4-12 are obtained by the Willgerodt-Kindler procedure. The oxothioamids 13-19 result as the intermediate products of the synthesis of thioamids 4-10. The compounds 4, 5, 8, 9, 11, 14 and 17 do not respond to Mycobacterium tuberculosis H37Rv. The thioamids 4, 8 and 11 are of slight toxicity (LD50 greater than 2.8 g/kg, albino-Swiss mice) and inhibit the Carrageenin oedema of the Wistar rat claw minor than phyenylbutazon and indometacin.
通过威尔格罗德特-金德勒方法获得了5-甲基、3,5-二甲基-1-苯基-4-吡唑硫代乙酸和3,5-二甲基-1-苯基-4-吡唑碳酸4-12的吗啉代物、N-甲基哌嗪代物、哌啶代物和吡咯烷代物。氧代硫酰胺13-19是硫酰胺4-10合成的中间产物。化合物4、5、8、9、11、14和17对结核分枝杆菌H37Rv无反应。硫酰胺4、8和11具有轻微毒性(LD50大于2.8 g/kg,瑞士白化小鼠),并且比苯基丁氮酮和吲哚美辛更能抑制Wistar大鼠爪的角叉菜胶性水肿。