Search Results - "Trapani, Angelo J"
-
1
Alternative Complement Pathway Inhibition With Iptacopan for the Treatment of C3 Glomerulopathy-Study Design of the APPEAR-C3G Trial
Published in Kidney international reports (01-10-2022)“…Complement 3 glomerulopathy (C3G) is a rare kidney disease characterized by dysregulation of the alternative pathway (AP) of the complement system. About 50%…”
Get full text
Journal Article -
2
Design and Synthesis of Potent, Selective Inhibitors of Endothelin-Converting Enzyme
Published in Journal of medicinal chemistry (23-04-1998)“…Endothelin-1 is the most potent peptidic vasoconstrictor discovered to date. The final step of posttranslational processing of this peptide is the conversion…”
Get full text
Journal Article -
3
BLOCKADE OF ALDOSTERONE PRODUCTION AS A NOVEL APPROACH TO THE MANAGEMENT OF HIGH BLOOD PRESSURE: EFFICACY AND TOLERABILITY OF THE ALDOSTERONE SYNTHASE INHIBITOR LCI699 IN PATIENTS WITH STAGE 1-2 HYPERTENSION
Published in Journal of the American College of Cardiology (09-03-2010)Get full text
Journal Article -
4
Potent and Selective Non-Peptidic Inhibitors of Endothelin-Converting Enzyme-1 with Sustained Duration of Action
Published in Journal of medicinal chemistry (10-02-2000)“…Potent and selective non-peptidic inhibitors of human endothelin-converting enzyme-1 (ECE-1) have been designed as potential modulators of endothelin (ET-1)…”
Get full text
Journal Article -
5
CGS 35601 and its Orally Active Prodrug CGS 37808 as Triple Inhibitors of Endothelin-converting Enzyme-1, Neutral Endopeptidase 24.11, and Angiotensin-converting Enzyme
Published in Journal of cardiovascular pharmacology (01-11-2004)“…CGS 35601 is a potent triple inhibitor of endothelinconverting enzyme-1, neutral endopeptidase 24.11, and angiotensinconverting enzyme. It inhibited the…”
Get full text
Journal Article -
6
CGS 34226, a thiol-based dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11
Published in Clinical science (1979) (01-08-2002)“…Endothelins (ETs) are potent vasoconstrictors and have been implicated in the pathogenesis of various cardiovascular and renal diseases. In contrast, atrial…”
Get more information
Journal Article -
7
-
8
Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1
Published in Bioorganic & medicinal chemistry letters (04-11-2002)“…Directed screening of metalloprotease inhibitors identified CGS 30084 ( 1) as a potent inhibitor of endothelin-converting enzyme-1 (ECE-1) in vitro (IC 50=77…”
Get full text
Journal Article -
9
Effects of the ECE/NEP inhibitor CGS 34225 on the big ET-1-induced pressor response and plasma atrial natriuretic peptide concentration in conscious rats
Published in Clinical science (1979) (01-08-2002)“…CGS 34226 is a thiol-containing, potent dual inhibitor of endothelin converting enzyme-1 (ECE-1) and neutral endopeptidase 24.11 (NEP) with IC(50) values of 11…”
Get more information
Journal Article -
10
-
11
N-Phosphonomethyl Dipeptides and Their Phosphonate Prodrugs, a New Generation of Neutral Endopeptidase (NEP, EC 3.4.24.11) Inhibitors
Published in Journal of medicinal chemistry (01-02-1994)“…Inhibitors of the zinc protease neutral endopeptidase (NEP, EC 3.4.24.11) offer significant therapeutic interest as antihypertensives due to their ability to…”
Get full text
Journal Article -
12
Design and Synthesis of a Potent and Selective Endothelin-Converting Enzyme Inhibitor, CGS 35066
Published in Journal of cardiovascular pharmacology (2000)“…CGS 26303 has previously been shown to inhibit human endothelin converting enzyme-1 (ECE-1) with an IC50 of 410 nM and to be efficacious in several animal…”
Get full text
Journal Article -
13
Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Published in Bioorganic & medicinal chemistry letters (04-09-2000)“…Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in…”
Get full text
Journal Article -
14
Pharmacological Properties of CGS 35066, a Potent and Selective Endothelin-Converting Enzyme Inhibitor, in Conscious Rats
Published in Journal of cardiovascular pharmacology (2000)“…The purpose of this study was to examine the pharmacologic properties of CGS 35066, a novel aminophosphonate inhibitor of endothelin-converting enzyme-1…”
Get full text
Journal Article -
15
Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors
Published in Bioorganic & medicinal chemistry letters (12-02-2001)“…Through directed screening of metalloprotease inhibitors, CGS 30084 (1) has been identified as a potent endothelin-converting enzyme-1 (ECE-1) inhibitor in…”
Get full text
Journal Article -
16
Iptacopan Reduces Proteinuria and Stabilizes Kidney Function in C3 Glomerulopathy
Published in Kidney international reports (01-10-2024)Get full text
Journal Article -
17
Mercaptoacyl Dipeptides as Orally Active Dual Inhibitors of Angiotensin-Converting Enzyme and Neutral Endopeptidase
Published in Journal of medicinal chemistry (02-08-1996)“…Dual inhibitors of the two zinc metallopeptidases, neutral endopeptidase (NEP, EC 3.4.24.11) and angiotensin-I-converting enzyme (ACE, EC 2.4.15.1), have been…”
Get full text
Journal Article -
18
Antihypertensive and natriuretic effects of CGS 30440, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase 24.11
Published in The Journal of pharmacology and experimental therapeutics (01-03-1998)“…Dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitors, by decreasing angiotensin-II production and by preventing the degradation of…”
Get more information
Journal Article -
19
New .alpha.-Thiol Dipeptide Dual Inhibitors of Angiotensin-I-Converting Enzyme and Neutral Endopeptidase EC 3.4.24.11
Published in Journal of medicinal chemistry (01-12-1995)“…Dual inhibitors of the two zinc metallopeptidases, neutral endopeptidase (NEP, EC 3.4.24.11) and angiotensin-I converting enzyme, have been the focus of much…”
Get full text
Journal Article -
20
Benzofused Macrocyclic Lactams as Triple Inhibitors of Endothelin-Converting Enzyme, Neutral Endopeptidase 24.11, and Angiotensin-Converting Enzyme
Published in Journal of cardiovascular pharmacology (1998)“…The purpose of this study was to identify endothelin-converting enzyme (ECE) inhibitors that also possess inhibitory activity for neutral endopeptidase 24.11…”
Get full text
Journal Article