A series of substituted glutaramides were synthesised using Candoxatrilat 1 as a lead and evaluated for potency against neutral endopeptidase (NEP) as a potential treatment for female sexual arousal disorder (FSAD). In this paper, we describe studies in which we were able to increase NEP activity substantially over the levels reported for previous compounds from this programme by appropriate substitution in both the P(1)(') and P(2)(') regions. Optimisation led to the 4-chlorophenpropylamide S-30 which was selected as a candidate for further study.
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http://dx.doi.org/10.1016/j.bmc.2006.10.002 | DOI Listing |
Indian Heart J
January 2025
Department of Community Medicine, Dr. S. N. Medical College, Jodhpur, India.
Angiotensin Receptor Neprilysin Inhibitor (ARNI) has not shown to be promising in Heart failure with preserved LVEF. Role of ARNI in Right ventricular systolic dysfunction with preserved LVEF needs to be evaluated. We took 50 patients with isolated RV systolic dysfunction and divided them into two groups of 25 patients each- Conventional treatment and ARNI in addition to conventional treatment.
View Article and Find Full Text PDFCytotechnology
February 2025
Department of Neurology, Hubei Provincial Hospital of Integrated Traditional and Western Medicine, Jianghan District, No. 11 Lingjiaohu Road, Wuhan, 430015 China.
Unlabelled: Alzheimer's disease (AD) is a progressive neurological condition that causes brain shrinkage and cell death. This study aimed to identify the role of the NORAD/miR-26b-5p axis in AD. StarBase was used to examine the binding sequences of miR-26b-5p to LncRNA NORAD or its target genes, which were verified by a double luciferase reporter assay.
View Article and Find Full Text PDFJ Mol Cell Cardiol Plus
March 2024
Institute of Experimental Pharmacology and Toxicology, University Medical Center Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg, Germany.
Sacubitril/valsartan (Sac/Val) belongs to the group of angiotensin receptor-neprilysin inhibitors and has been used for the treatment of heart failure (HF) for several years. The mechanisms that mediate the beneficial effects of Sac/Val are not yet fully understood. In this study we investigated whether Sac/Val influences the two proteolytic systems, the ubiquitin-proteasome system (UPS) and the autophagy-lysosomal pathway (ALP), in a mouse model of pressure overload induced by transverse aortic constriction (TAC) and in human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) treated with endothelin-1 (ET1) serving as a human cellular model of hypertrophy.
View Article and Find Full Text PDFJACC Adv
January 2025
Heart Failure Clinics, Instituto do Coracao, Hospital das Clínicas HCFMUSP, Faculdade de Medicina, Universidade de Sao Paulo, Sao Paulo, Sao Paulo, Brazil.
Background: Worsening heart failure (WHF) challenges health care with frequent rehospitalizations and reduced quality of life for patients. Despite therapeutic advances, high rehospitalization risks highlight the urgent need for new treatments.
Objectives: This study evaluated the effectiveness of initiating novel therapies during hospitalization or vulnerable phase for WHF patients to reduce rehospitalization risks and determine the optimal treatment sequence.
Medicine (Baltimore)
January 2025
Faculty of Chinese Medicine, Macau University of Science and Technology, Taipa, Macau, China.
Rationale: Thrombotic microangiopathies (TMA) caused by malignant hypertension is an acute and critical disease among rare diseases. Although renal biopsy pathology is a golden indicator for diagnosing kidney disease, it cannot distinguish between primary and secondary TMA and requires a comprehensive diagnosis in conjunction with other laboratory tests and medical history.
Patient Concerns: A 33-year-old young man was hospitalized due to unexplained kidney failure.
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