Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H 3 receptor inverse agonists

…, D Tsukahara, S Ito, T Tanaka, N Takenaga…

Index: Jitsuoka, Makoto; Tsukahara, Daisuke; Ito, Sayaka; Tanaka, Takeshi; Takenaga, Norihiro; Tokita, Shigeru; Sato, Nagaaki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5101 - 5106

Full Text: HTML

Citation Number: 21

Abstract

Spiro-isobenzofuranones 1a and 1b were discovered as potent, selective, and brain- penetrable non-imidazole H3 receptor inverse agonists. Our corporate sample collection was screened to identify 2a as a lead. Recognizing the right-hand portion of 2a as an essential pharmacophore, an extensive screen of the left-hand piperidine portion was carried out to yield the potent spiro-derivatives 2t− x. Spiro-isobenzofuranone 2x, the most ...