220191-09-3Relevant academic research and scientific papers
4-Benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists
Wijtmans, Maikel,Celanire, Sylvain,Snip, Erwin,Gillard, Michel R.,Gelens, Edith,Collart, Philippe P.,Venhuis, Bastiaan J.,Christophe, Bernard,Hulscher, Saskia,Van Der Goot, Henk,Lebon, Florence,Timmerman, Henk,Bakker, Remko A.,Lallemand, Bénédicte I. L. F.,Leurs, Rob,Talaga, Patrice E.,De Esch, Iwan J. P.
supporting information; experimental part, p. 2944 - 2953 (2009/04/11)
Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R agonists have received less attention despite their potential use in s
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: Novel antagonists of the histamine H3 receptor
Aslanian, Robert,Brown, Joan E.,Shih,Wa Mutahi, Mwangi,Green, Michael J.,She, Susan,Del Prado, Maurice,West, Robert,Hey, John
, p. 2263 - 2268 (2007/10/03)
A series of amidine substituted phenyl-, benzyl-, and phenethylimidazoles based on the known H3 against SKandF 91606 (4) has been synthesized and tested as ligands for the histamine H3 receptor. Insertion of a phenyl ring between the imidazole ring and the amidine moiety produces antagonists. The benzyl series was found to be the most potent and was further investigated. Compounds 9c and 18 (entries 5 and 12, Table 1) are potent ligands for the H3 receptor with K(i) values of 16 nM and 7.2 nM respectively. In vivo, both compounds were shown to be equipotent to thioperamide (2), the standard H3 antagonist.
