Modifications of 4-Amino-substituted 5-Phenyl-3-(trifluoromethyl)pyrazoles for the Development of New Analgesics,ChemistrySelect

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Modifications of 4-Amino-substituted 5-Phenyl-3-(trifluoromethyl)pyrazoles for the Development of New Analgesics
ChemistrySelect ( IF 1.9 ) Pub Date : 2023-12-13 , DOI: 10.1002/slct.202303265
Evgeny V. Shchegolkov ₁ , Anastasia N. Perminova ₁ , Natalia A. Malkova ₁ , Svetlana O. Kushch ₁ , Yanina V. Burgart ₁ , Galina A. Triandafilova ₂ , Sergey Yu. Solodnikov ₂ , Olga P. Krasnykh ₂ , Victor I. Saloutin ₁

Affiliation

A series of 4-(het)arylimino-3-(trifluoromethyl)-5-phenylpyrazoles was synthesized. Alkylation of 4-aminopyrazoles with methylating agents and butyl bromide was investigated. The addition of phenylisothiocyanate to 4-aminopyrazoles to give compounds with a thiourea fragment. All derivatives of aminopyrazoles have an acceptable ADME profile. Using the “hot plate” test in vivo, the analgesic activity of synthesized pyrazoles was evaluated. The most active compound was 1-phenyl-N-(5-phenyl-3-(trifluoromethyl)pyrazol-4-yl)methanimine.

中文翻译：

4-氨基取代的 5-苯基-3-(三氟甲基)吡唑的修饰用于开发新型镇痛药

合成了一系列4-(杂)芳基亚氨基-3-(三氟甲基)-5-苯基吡唑。研究了 4-氨基吡唑与甲基化剂和丁基溴的烷基化。将异硫氰酸苯酯加成到 4-氨基吡唑上，得到带有硫脲片段的化合物。所有氨基吡唑衍生物都具有可接受的 ADME 特征。采用体内“热板”试验评价合成吡唑类化合物的镇痛活性。最活跃的化合物是1-苯基-N-(5-苯基-3-(三氟甲基)吡唑-4-基)甲胺。

更新日期：2023-12-16

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