1026219-94-2Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationships of novel non- imidazole histamine H3 receptor antagonists
Linney, Ian D.,Buck, Ildiko M.,Harper, Elaine A.,Kalindjian, S. Barret,Pether, Michael J.,Shankley, Nigel P.,Watt, Gillian F.,Wright, Paul T.
, p. 2362 - 2370 (2007/10/03)
Novel, potent, and selective non-imidazole histamine H3 receptor antagonists have been prepared based on the low-affinity ligand dimaprit (pK(I) 7.32 ± 0.12, pK(B) 5.93 ± 0.17). Detailed structure-activity studies have revealed that N-(4-chlorobenzyl)-N-(6-pyrrolidin-1-ylhexyl)guanidine (pK(I) 8.38 ± 0.21, pK(B) 8.39 ± 0.13), 30, and N-(4-chlorobenzyl)-N-(7- pyrrolidin-1-ylheptyl)guanidine (pK(I) 8.78 ± 0.12, pK(B) 8.38 ± 0.10), 31, exhibit high affinity for the histamine H3 receptor. Antagonists 30 and 31 demonstrate significant selectivity over the other histamine, H1 and H2, receptor subtypes and a 100-fold selectivity in the σ1 binding assay. Compounds 30 and 31 are the most potent, selective non-imidazole histamine H3 receptor antagonists reported in the literature to date.
