Design, synthesis, and structure− activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and …
AJ Hirsh, BF Molino, J Zhang… - Journal of medicinal …, 2006 - ACS Publications
Amiloride (1), the prototypical epithelial sodium channel (ENaC) blocker, has been
administered with limited success as aerosol therapy for improving pulmonary function in
patients with the genetic disorder cystic fibrosis. This study was conducted to synthesize and
identify more potent, less reversible ENaC blockers, targeted for aerosol therapy and
possessing minimal systemic renal activity. A series of novel 2-substituted acylguanidine
analogues of amiloride were synthesized and evaluated for potency and reversibility on …
administered with limited success as aerosol therapy for improving pulmonary function in
patients with the genetic disorder cystic fibrosis. This study was conducted to synthesize and
identify more potent, less reversible ENaC blockers, targeted for aerosol therapy and
possessing minimal systemic renal activity. A series of novel 2-substituted acylguanidine
analogues of amiloride were synthesized and evaluated for potency and reversibility on …
