[Design, synthesis and insulin-sensitizing activity of some peroxisome proliferator-activated gamma agonists].

Yao Xue Xue Bao

R&D Department, Chengdu Di'ao Pharmaceutical Group Co., LTD, Chengdu 610041, China.

Published: February 2005


Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

Aim: To find new peroxisome proliferator-activated y agonists with high activity and low toxicity.

Methods: Based on JTT-501 and JTT-20993, new isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds were designed and synthesized. Their insulin-sensitizing activities were evaluated.

Results: Eight new compounds were obtained. The structures of synthesized compounds were characterized by NMR, MS and IR. Four compounds (1A-4A) showed insulin-sensitizing activities.

Conclusion: Compounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.

Download full-text PDF

Source

Publication Analysis

Top Keywords

peroxisome proliferator-activated
8
insulin-sensitizing activities
8
compounds
5
[design synthesis
4
insulin-sensitizing
4
synthesis insulin-sensitizing
4
insulin-sensitizing activity
4
activity peroxisome
4
proliferator-activated gamma
4
gamma agonists]
4

Similar Publications

MR409, a synthetic growth hormone-releasing hormone (GHRH) analogue, has demonstrated therapeutic potential in enhancing islet cell transplantation efficacy in diabetes mice and exerts beneficial effects on cardiovascular diseases. The present study investigated the renoprotective effects of MR409 on db/db and streptozotocin (STZ)-induced diabetic mice, focusing on its role in modulating oxidative stress and ferroptosis. db/db or STZ mice combined with high fat diet were used to establish the type 2 diabetic models.

View Article and Find Full Text PDF

Neonatal sevoflurane exposure disrupted fatty acids metabolism, leading to hypomyelination and neurological impairments.

Biomed Pharmacother

September 2025

Department of Anesthesiology, The Second Hospital of Hebei Medical University, Shijiazhuang, Hebei, China; Hebei Key Laboratory of Neurodegenerative Disease Mechanism, Shijiazhuang, Hebei, China; Key Laboratory of Clinical Neurology, Ministry of Education, Hebei Medical University, Shijiazhuang, Heb

Myelin is a lipid-rich substance that is crucial for neural function. Neonatal anesthesia has been linked to neurological impairments associated with myelination dysfunction. This study sought to evaluate whether disrupted fatty acid homeostasis is involved in the mechanism of sevoflurane developmental neurotoxicity.

View Article and Find Full Text PDF

Background: We conducted a transcriptomic analysis to examine cerebellar transcriptional changes in a mouse model of chronic intermittent alcohol exposure.

Methods: We established a mouse model of chronic intermittent alcohol exposure and conducted a cerebellar transcriptomic analysis. After identifying differentially expressed genes, we analyzed pathway enrichment using the Kyoto Encyclopedia of Genes and Genomes and Gene Ontology.

View Article and Find Full Text PDF

Adrenal lipoma formation via PI(3,4,5)P/AKT-dependent transdifferentiation of adrenocortical cells into adipocytes.

Proc Natl Acad Sci U S A

September 2025

Department of Biochemical Pathophysiology, Medical Research Laboratory, Institute of Integrated Research, Institute of Science Tokyo, Yushima, Bunkyo-ku, Tokyo 113-8510, Japan.

Adrenal lipomas are benign tumors containing ectopic adipose tissue in the adrenal gland, an organ that normally lacks both adipocytes and their progenitors. The origin of this ectopic fat remains enigmatic, and the absence of a genetic animal model has hindered its investigation. Phosphatidylinositol 3,4,5-trisphosphate [PI(3,4,5)P], a key signaling lipid that regulates cellular growth and differentiation, is tightly regulated by the lipid phosphatases PTEN (phosphatase and tensin homolog) and SHIP2 (SH2-containing inositol phosphatase 2).

View Article and Find Full Text PDF

Chrysanthemum morifolium Ramat. water extract prevents and treats metabolic-associated fatty liver disease via pan-PPAR activity.

J Ethnopharmacol

September 2025

School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China; Anhui Province Key Laboratory of Research & Development of Chinese Medicine, Hefei, Anhui 230012, China. Electronic address:

Ethnopharmacological Relevance: Chrysanthemum (Chrysanthemum morifolium Ramat.) is a widely used plant with both medicinal and dietary applications, boasting a history spanning thousands of years, exhibiting various pharmacological activities such as anti-inflammatory, antipyretic, antibacterial, and antiviral effects. According to the Compendium of Materia Medica, chrysanthemum is renowned for its ability to calm the liver and improve vision.

View Article and Find Full Text PDF