Title of article :
Aminoimidazoles as bioisosteres of acylguanidines: novel, potent, selective and orally bioavailable inhibitors of the sodium hydrogen exchanger isoform-1
Author/Authors :
Saleem Ahmad، نويسنده , , Khehyong Ngu، نويسنده , , Donald W. Combs، نويسنده , , Shung C. Wu، نويسنده , , David S. Weinstein، نويسنده , , Wen Liu، نويسنده , , Bang-Chi Chen، نويسنده , , Gamini Chandrasena، نويسنده , , Charles R. Dorso، نويسنده , , Mark Kirby، نويسنده , , Karnail S. Atwal، نويسنده ,
Abstract :
Inhibition of the sodium hydrogen exchanger isoform-1 (NHE-1) has been shown to limit damage to the myocardium under ischemic conditions in animals. While most known NHE-1 inhibitors are acylguanidines, this report describes the design and synthesis of a series of heterocyclic inhibitors of NHE-1 including aminoimidazoles with undiminished in vitro activity and oral bioavailability.