Semisynthesis of Nocarterphenyl A and Its Analogues.

J Nat Prod

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China.

Published: December 2024

-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).

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jnatprod.4c01198DOI Listing

Publication Analysis

Top Keywords

μm lower
8
semisynthesis nocarterphenyl
4
nocarterphenyl analogues
4
analogues -terphenyl
4
-terphenyl compounds
4
compounds possess
4
possess diverse
4
diverse range
4
range biological
4
biological activities
4

Similar Publications

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 PDF

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 PDF

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.

View Article and Find Full Text PDF

Quality of Life in Subcutaneous or Transvenous Implantable Cardioverter-Defibrillator Patients: A Secondary Analysis of the PRAETORIAN Trial.

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.).

Article Synopsis
  • The S-ICD was created to eliminate lead-related issues found in the TV-ICD, as it is an external device that sits under the skin rather than using leads inside the body.
  • This analysis comes from the PRAETORIAN trial, where patients were randomly assigned to either S-ICD or TV-ICD and assessed for quality of life through various questionnaires at different stages.
  • Results showed no significant differences in physical and mental well-being between the groups, but patients who experienced a shock recently reported lower social functioning and emotional health compared to those who did not.
View Article and Find Full Text PDF
Article Synopsis
  • Metabolic syndrome (MetS) is a significant global cardiovascular risk, and this study examined how the age at menarche (AAM) impacts MetS and its components across different generations of women.
  • The research involved 5,500 women from the Tehran Lipid and Glucose Study, categorizing them by birth cohorts and AAM, and utilized logistic regression to analyze the relationship between AAM and MetS prevalence.
  • Results indicated that early menarche (≤ 11 years) increases the risk of MetS, particularly in older generations, while late menarche (≥ 16 years) appears protective against certain metabolic issues, highlighting generational differences in AAM's impact on metabolic health.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!