A new class of analgesic agents toward prostacyclin receptor inhibition: Synthesis, biological studies and QSAR analysis of 1-hydroxyl-2-substituted phenyl-4, 4, 5, 5- …

…, L Peng, YR Tang, C Wang, Z Zhang, S Peng

Index: Zhao, Ming; Li, Zheng; Peng, Li; Tang, Yu-Rong; Wang, Chao; Zhang, Ziding; Peng, Shiqi European Journal of Medicinal Chemistry, 2008 , vol. 43, # 5 p. 1048 - 1058

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Citation Number: 15

Abstract

By studying the structural similarity of analgesic imidazolines and 2-phenylnitronyl nitroxides, 20 1-hydroxyl-2-substituted phenyl-4, 4, 5, 5-tetramethylimidazolines (2a–t) were newly synthesized as selective antagonists of prostacyclin receptor (IP receptor). In the in vivo tail-flick assay, 2a–t (dose, 0.13 mmol/kg) receiving mice showed increased pain thresholds ranging from 20.52±7.25% to 90.94±11.97%, which were significantly higher ...