Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists

…, Q Sun, L Schmid, KJ Valenzano, Y Rotshteyn…

Index: Tafesse, Laykea; Sun, Qun; Schmid, Lori; Valenzano, Kenneth J.; Rotshteyn, Yakov; Su, Xin; Kyle, Donald J. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5513 - 5519

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Citation Number: 39

Abstract

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 ...