Utilizing X-ray crystal structure analysis, (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides were designed and identified as renin inhibitors. The most potent compound 15 demonstrated favorable pharmacokinetic and pharmacodynamic profiles in rat.
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http://dx.doi.org/10.1016/j.bmcl.2012.09.103 | DOI Listing |
Front Pharmacol
January 2025
TCM Regulating Metabolic Diseases Key Laboratory of Sichuan Province, Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Background: Diabetic kidney disease (DKD) has become the leading cause of end-stage renal disease in the world. However, the current conventional approaches have not yet achieved satisfactory efficacy. As one of the most influential products in botanical medicine, L.
View Article and Find Full Text PDFCurr Probl Cardiol
January 2025
Departamento de Cardiología, Clínica Las Américas Auna. Medellín, Colombia.
Background: Despite recommendations from clinical practice guidelines to initiate four drug classes in patients with heart failure (HF) with reduced ejection fraction, information on real-world implementation remains limited. This study evaluated the medications initiated and titrated, the time until the optimal treatment tolerated, pharmacological profiles, patient's adherence, and causes of non-use of guideline directed-medical therapy (GDMT) in a cohort of patients with HF.
Methods: A retrospective cohort study was conducted on patients treated in a heart failure program in Colombia.
Transplant Proc
January 2025
Doctor Peset Aleixandre University Hospital, Valencia, Spain; Fisabio Foundation, Valencia, Spain; University of Valencia, Valencia, Spain.
Background: The potential anti-proteinuric effect of sodium-glucose cotransporter-2 inhibitors (SGLT2i) is of special interest in kidney transplantation. Its benefits have been demonstrated in diabetic kidney transplant recipients (KTRs). We analyzed the efficacy and safety of SGLT2i in non-diabetic KTRs collecting clinical and analytical data at baseline and 6 months after the introduction of the drug.
View Article and Find Full Text PDFCurr Cardiol Rep
January 2025
Pediatric Advanced Heart Failure and Heart Transplant Program, University of Mississippi Medical Center, 2500 N State Street, Jackson, MS, USA.
Purpose Of Review: Traditionally viewed as a passive player in circulation, the right ventricle (RV) has become a pivotal force in hemodynamics. RV failure (RVF) is a recognized complication of primary cardiac and pulmonary vascular disorders and is associated with a poor prognosis. Unlike treatments for left ventricular failure (LVF), strategies such as adrenoceptor signaling inhibition and renin-angiotensin system modulation have shown limited success in RVF.
View Article and Find Full Text PDFAm J Physiol Heart Circ Physiol
January 2025
Amsterdam University Medical Centers, Vrije Universiteit Amsterdam, Department of Cardiology, Amsterdam, The Netherlands.
The acute response to therapeutic afterload reduction differs between heart failure with preserved (HFpEF) versus reduced ejection fraction (HFrEF), with larger left ventricular (LV) stroke work augmentation in HFrEF compared to HFpEF. This may (partially) explain the neutral effect of HFrEF-medication in HFpEF. It is unclear whether such differences in hemodynamic response persist and/or differentially trigger reverse remodeling in case of long-term afterload reduction.
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