TRPV1 modulators: Synthesis and in vitro evaluation of 1-heteroaryl piperidinecarboxamide and piperazinylurea derivatives.
作者： Cenzo Congiu , Valentina Onnis , Gianfranco Balboni , Aniello Schiano-Moriello , Vincenzo Di Marzo
DOI: 10.1016/J.EJMECH.2015.05.041
关键词: Recombinant DNA 、 Structure–activity relationship 、 Antagonist 、 Agonist 、 Chemistry 、 Stereochemistry 、 Potency 、 TRPV1 、 In vitro 、 HEK 293 cells
摘要: A series of new 1-heteroaryl piperidinecarboxamide and piperazinylurea derivatives was synthesized evaluated as TRPV1 modulators in a Ca(2+) channel assay HEK-293 cells overexpressing the human recombinant channel. Structural variations putative key portions molecules afforded several compounds endowed with agonist and/or antagonist/desensitizing activity at low micromolar concentration. As promising examples from this series, piperidine-3-carboxamide derivative 31 exerts agonist/desensitizing concentration, while 39 41 act antagonists sub-micromolar potency.
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