98331-33-0Relevant academic research and scientific papers
New Antihistaminic N-Heterocyclic 4-Piperidinamines. 3. Synthesis and Antihistaminic Activity of N-(4-Piperidinyl)-3H-imidazopyridin-2-amines
Janssens, Frans,Torremans, Joseph,Janssen, Marcel,Stokbroekx, Raymond A.,Luyckx, Marcel,Janssen, Paul A. J.
, p. 1943 - 1947 (2007/10/02)
To study the bioisosteric replacement of a 2-pyridyl ring for a phenyl nucleus in astemizole, a series of N-(4-piperidinyl)-3H-imidazopyridin-2-amines was synthesised and evaluated.The title compounds were obtained starting from either 8a or 8b by four synthetic methods.The in vivo antihistamine activity was evaluated by the compound 48/80-induced lethality test in rats and the histamine-induced lethality test in guinea pigs after oral and/or subcutaneous administration.Compound 37, the isostere of astemizole, showed the most potent antihistaminic properties in the rat.However, astemizole is superior to 37 as to duration of action and total potency.
