-Terphenyl compounds are known to possess a diverse range of biological activities, making the synthesis of novel -terphenyl derivatives a significant research objective. In this study, we report the first synthesis of nocarterphenyl A (), characterized by a thiazole-fused -terphenyl framework. Furthermore, we synthesized 18 additional analogs, including the naturally occurring compound 5-methoxy-4,7-bis(4-methoxyphenyl)benzo[]thiazol-6-ol (), employing a similar synthetic approach. Notably, compounds , , -, and demonstrated potent inhibitory effects against protein tyrosine phosphatase 1B (PTP1B), exhibiting IC values ranging from 2.2 to 7.9 μM, which are lower than that of oleanolic acid (13.2 μM). Additionally, compound was found to inhibit α-glucosidase from human colorectal adenocarcinoma (Caco-2) cells with an IC value of 10.4 μM, which is also lower than that of acarbose (11.2 μM).
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http://dx.doi.org/10.1021/acs.jnatprod.4c01198 | DOI Listing |
Am J Cardiovasc Drugs
December 2024
Department of Internal Medicine, Western Michigan University Homer Stryker M.D. School of Medicine, 1000 Oakland Dr, Kalamazoo, MI, USA.
Reducing low-density lipoprotein cholesterol (LDL-C) levels has been shown to reduce the risk of developing atherosclerotic cardiovascular disease (ASCVD). Statins are the foundation of LDL-C lowering therapy with other non-statin agents used in circumstances where goal LDL-C levels are not reached or owing to intolerance to adverse effects of statins. In 2003, the discovery of the role of the proprotein convertase subtilisin/kexin type 9 (PCSK9) system in promoting elevated LDL-C levels led to new avenues of drug development to achieve target LDL-C.
View Article and Find Full Text PDFMaterials (Basel)
December 2024
Department of Civil Engineering, Toronto Metropolitan University, Toronto, ON M5B 2K3, Canada.
This study presents a comprehensive assessment of the fresh state, rheological, and mechanical properties of alkali-activated mortars (AAMs) developed by incorporating magnesium oxide (MgO) and nanomaterials. A total of 24 AAM mixes with varying content of MgO, multi-walled carbon nanotube (MWCNT), and reduced graphene oxide (rGO) were developed following the one-part dry mix technique using powder-based activators/reagents. The effects of the types/combinations of source materials (binary or ternary)/reagents, MgO (0 to 5%), MWCNT (0 to 0.
View Article and Find Full Text PDFAm Heart J
November 2024
From the Cardiovascular Critical Care Unit, National Institute of Cardiology Ignacio Chávez, Mexico City, México. Electronic address:
Background: Coronary artery ectasia (CAE) of the culprit infarct artery is a rare finding in patients with acute coronary syndrome (ACS). While anticoagulants have been suggested to reduce recurrent events, the optimal antithrombotic therapy remains unclear.
Methods: OVER-TIME was an open label, exploratory, randomized controlled trial comparing dual antiplatelet therapy (DAPT; acetyl-salicylic-acid 100mg plus clopidogrel 75mg daily) versus single antiplatelet (SAPT, clopidogrel 75mg) plus DOAC (rivaroxaban 15mg) in patients with ACS and CAE.
Circ Cardiovasc Qual Outcomes
November 2024
Department of Cardiology, Amsterdam Cardiovascular Sciences Heart Failure and Arrhythmias, Amsterdam University Medical Centers Location University of Amsterdam, Heart Center, the Netherlands (R.E.K., J.A.d.V., L.V.A.B., T.F.B., S.P., A.-F.B.E.Q., L.S., W.v.d.S., A.d.W., J.R.d.G., K.M.K., J.G.P.T., A.A.M.W., L.R.A.O.N.).
Endocrinol Diabetes Metab
November 2024
Reproductive Endocrinology Research Center, Research Institute for Endocrine Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
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