Bioisosteric transformation of H1-antihistaminic benzimidazole derivatives.
With the aim of obtaining new H1-antihistaminic agents, transformations of previously reported antihistaminic benzimidazoles were performed on the basis of the concept of bioisosterism. Among the compounds prepared, imidazo[4,5-b]pyridine (8) and 4(3H)-quinazolinone (11) exhibited significant H1-antihistaminic activity.
Iemura
R
R
Hori
M
M
Saito
T
T
Ohtaka
H
H
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D007536:Isomerism; D009130:Muscle, Smooth / Q000187:drug effects
D001562:Benzimidazoles; D006634:Histamine H1 Antagonists