93836-41-0Relevant academic research and scientific papers
Angiotensin-converting enzyme inhibitors. 9. Novel [[N-(1-carboxy-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity
Barton,Piwinski,Skiles,Regan,Menard,Desai,Golec,Reilly,Goetzen,Ueng,Warus,Schwab,Samuels,Neiss,Suh
, p. 1600 - 1606 (2007/10/02)
A series of molecules 1 having sulfonamide diuretic moieties covalently linked to non-sulfhydryl angiotensin-converting enzyme inhibitors (ACEI) were prepared and tested for both activities. IC50 values for ACEI as low as 7 nM were observed. Di
Angiotensin Converting Enzyme Inhibitors: Spirapril and Related Compounds
Smith, Elizabeth M.,Swiss, Gerald F.,Neustadt, Bernard R.,McNamara, Paul,Gold, Elijah H.,et al.
, p. 1600 - 1606 (2007/10/02)
The synthesis of spirapril (5), spiraprilat (25), their RSS stereoisomers, and their glycyl (18b) and lysyl (36, 37) analogues is described.These compounds were evaluated in vivo for inhibition of angiotensin converting enzyme (ACE), and selected compounds were evaluated for in vitro ACE inhibition (spirapril ID50 16 μg/kg; spiraprilat IC50 0.8 nM, ID50 8 μg/kg).In anesthetized rats, iv, esters 5 and 36 are more potent than enalapril, and diacids 25 and 37 are more potent than enalaprilat in vitro.In the conscious rats, orally, 5 and enalapril (2) showed potent and sustained activity at doses of 0.03-1 and 0.1-1 mg/kg, respectively.From this work, spirapril was selected for clinical evaluation as an antihypertensive agent.
