Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.

  title={Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.},
  author={Laykea Tafesse and Qun Sun and Lori A Schmid and Kenneth J. Valenzano and Yakov Rotshteyn and Xin Su and Donald J Kyle},
  journal={Bioorganic & medicinal chemistry letters},
  volume={14 22},
A structurally biased chemical library of pyridazinylpiperazine analogs was prepared in an effort to improve the pharmaceutical and pharmacological profile of the lead compound N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide (BCTC). The library was evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH5.5-induced (pH) FLIPR assays in a human VR1-expressing HEK293 cell line. The most potent VR1 antagonists were found to have IC(50) values… CONTINUE READING

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