Document Report Card

ID: ALA1121553

Journal: J Med Chem

Title: Substituted 6,7-dihydroimidazo[1,2-a]purin-9(4H)-ones.

Authors: Temple DL, Yevich JP, Catt JD, Owens D, Hanning C, Covington RR, Seidehamel RJ, Dungan KW.

Abstract: The synthesis of a series of substituted 6,7-dihydroimidazo[1,2-a]purin-9(4H)-ones is described. Several members of the series exhibit enhanced antiallergic and bronchodilator activity and reduced side effects as compared to theophylline. Structure-activity relationships and metabolic considerations are discussed for the series. Analogues substituted with a 4-(4-chlorobenzyl) moiety, such as 33 and 40, shown an optimal balance of antiallergic and bronchodilator activity and are of particular interest. Compound 33 is significantly more potent than theophylline against both metacholine- and antigen-induced bronchospasms, does not affect spontaneous motor activity, and shows minimal cardiovascular effects in the rat.

CiteXplore: 6161252

DOI: 10.1021/jm00185a008