Pivalopril, a novel orally active angiotensin-converting enzyme inhibitor, acts by blocking the conversion of angiotensin I to angiotensin II.

Pivalopril, a novel compound featuring a hindered sulfur group, exhibits promising properties as an orally effective angiotensin-converting enzyme (ACE) inhibitor and antihypertensive agent, showcasing superior effects compared to Captopril in various studies. When administered to conscious normotensive dogs and spontaneously hypertensive rats (SHR), Pivalopril demonstrates dose-related antagonism of angiotensin I (AngI) pressor effects and a notable reduction in mean arterial pressure, highlighting its potency and effectiveness at incremental doses ranging from 0.01-1.0 mg/kg orally. Notably, when dosed at 100 mg/kg per day, Pivalopril outperforms Captopril in lowering mean arterial pressure. The ED50 values for Pivalopril and Captopril further affirm its competitive efficacy in both dogs and rats. Furthermore, Pivalopril shows a similar duration of action to Captopril at equieffective doses, underscoring its potential as a potent antihypertensive treatment option.