Synthesis and sedative activity of 5-(4'-β-D-allopyranosyloxyphenyl)-3-aryl- 4,5-dihydropyrazole-1-carbothioamides
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5-(4'-β-D-Allopyranosyloxyphenyl)-3-aryl-4,5-dihydropyrazole-1-carbothioamides (2a–2h) were synthesized by the reaction of (1a–1h) with thiosemicarbazide and KOH in ethanol. The structures of all new compounds were characterized by 1HNMR, IR, and MS (HR-MS) spectra. A preliminary bioassay test of 1f–1h and 2a–2h suggested that most of these helicid analogues showed mild to strong activity. Compounds 1g, 2a, 2c, and 2f at a dose of 200 mg·kg–1 were better than that of the parent helicid.
Keywordshelicid Claisen-Schmidt reaction pyrazoline carbothioamide
We thank the Analytical & Testing Center of Sichuan University, P. R. China for assistance in obtaining analytical data.
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