Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists

…, CE Tedford, R Gregory, MK Handley…

Index: Ali, Syed M.; Tedford, Clark E.; Gregory, Rosilyn; Handley, Michael K.; Yates, Stephen L.; Hirth, Walter W.; Phillips, James G. Journal of Medicinal Chemistry, 1999 , vol. 42, # 5 p. 903 - 909

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Citation Number: 71

Abstract

New, potent, and selective histamine H3 receptor antagonists have been synthesized by employing the use of (1) an appropriately positioned nonpolar acetylene spacer group,(2) either a two-carbon straight chain linker or a conformationally restricting trans-cyclopropane ring between the C-4 position of an imidazole headgroup and the acetylene spacer, and (3) a Topliss operational scheme for side-chain substitution for optimizing the hydrophobic ...