A series of novel 2-(diarylalkyl)aminobenzothiazoles were designed based on commercial synthetic calcium channel blockers (CCBs) and angiotensin converting enzyme (ACE) inhibitors. Which are further modified based on the natural products which are angiotensin converting enzyme (ACE) inhibitors. Completely green protocol was developed for their synthesis. As they are initially designed based on CCBs, they were screened for their ACE inhibition property believing that almost all the compounds will be CCBs. Out of 42 compounds two lead molecules were identified as ACE inhibitors, which were further screened for CCB. As expected both were identified as CCBs with different selectivity over ACE inhibition. Their selectivity over ACE and CCB can be used to treat resistant hypertension.
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http://dx.doi.org/10.1016/j.ejmech.2014.06.035 | DOI Listing |
Neuropsychopharmacol Rep
March 2025
Molecular Psychoneuroimmunology, Institute for Genetic Medicine, Hokkaido University, Sapporo, Hokkaido, Japan.
COVID-19 exhibits not only respiratory symptoms but also neurological/psychiatric symptoms rarely including delirium/psychosis. Pathological studies on COVID-19 provide evidence that the cytokine storm, in particular (epidermal growth factor) EGF receptor (EGFR, ErbB1, Her1) activation, plays a central role in the progression of viral replication and lung fibrosis. Of note, SARS-CoV-2 virus (specifically, S1 spike domain) mimics EGF and directly transactivates EGFR, preceding the inflammatory process.
View Article and Find Full Text PDFComput Biol Med
January 2025
Department of Chemical and Biological Engineering, University at Buffalo, The State University of New York, Buffalo, NY, 14260, USA; Department of Biomedical Engineering, University at Buffalo, The State University of New York, Buffalo, NY, 14260, USA; Institute for Artificial Intelligence and Data Science, University at Buffalo, The State University of New York, Buffalo, NY, 14260, USA; Witebsky Center for Microbial Pathogenesis and Immunology, University at Buffalo, The State University of New York, Buffalo, NY, 14203, USA; Department of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, 14215, USA. Electronic address:
Patient-specific premorbidity, age, and sex are significant heterogeneous factors that influence the severe manifestation of lung diseases, including COVID-19 fibrosis. The renin-angiotensin system (RAS) plays a prominent role in regulating the effects of these factors. Recent evidence shows patient-specific alterations of RAS peptide homeostasis concentrations with premorbidity and the expression level of angiotensin-converting enzyme 2 (ACE2) during COVID-19.
View Article and Find Full Text PDFPLoS One
January 2025
Immunology and Immunotherapy Division, Center of Molecular Immunology (CIM), Havana, Cuba.
SARS-CoV-2 has continued spreading around the world in recent years since the initial outbreak in 2019, frequently developing into new variants with greater human infectious capacity. SARS-CoV-2 and its mutants use the angiotensin-converting enzyme 2 (ACE2) as a cellular entry receptor, which has triggered several therapeutic strategies against COVID-19 relying on the use of ACE2 recombinant proteins as decoy receptors. In this work, we propose an ACE2 silent Fc fusion protein (ACE2-hFcLALA) as a candidate therapy against COVID-19.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
Feinberg School of Medicine, Northwestern University, Chicago, IL, USA.
Background: Angiotensin-converting enzyme (ACE) is a validated risk locus for developing late-onset Alzheimer's disease (LOAD). ACE1 controls blood pressure through the renin-angiotensin system (RAS), but it is also present and acts locally in the brain. Hypertension is associated with an increased risk for developing AD, and people taking select RAS-targeting therapeutics have reduced incidence of AD.
View Article and Find Full Text PDFBackground: Seizures, traumatic brain injury (TBI), and dementia increase in prevalence with age. However, the role of seizure and TBI on cognitive impairment risk (CI) is unclear. This study investigated how a diagnosis of seizures and TBI was associated with the progression to CI and assessed the role of medications.
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