Research progress of indole compounds with potential antidiabetic activity

Y Zhu, J Zhao, L Luo, Y Gao, H Bao, P Li… - European Journal of …, 2021 - Elsevier
New types of antidiabetic agents are continually needed with diabetes becoming the
epidemic in the world. Indole alkaloids play an important role in natural products owing to …

Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators

C Pirat, A Farce, N Lebègue, N Renault… - Journal of medicinal …, 2012 - ACS Publications
Metabolic syndrome (MS) remains one of the leading causes of mortality in Western
societies and has become a major public health challenge worldwide. 1 The term metabolic …

Partial agonists activate PPARγ using a helix 12 independent mechanism

JB Bruning, MJ Chalmers, S Prasad, SA Busby… - Structure, 2007 - cell.com
Binding to helix 12 of the ligand-binding domain of PPARγ is required for full agonist activity.
Previously, the degree of stabilization of the activation function 2 (AF-2) surface was thought …

Novel hybrids of benzothiazole-1, 3, 4-oxadiazole-4-thiazolidinone: Synthesis, in silico ADME study, molecular docking and in vivo anti-diabetic assessment

R Bhutani, DP Pathak, G Kapoor, A Husain… - Bioorganic chemistry, 2019 - Elsevier
A series of new benzothiazole-1, 3, 4-oxadiazole-4-thiazolidinone hybrid analogs (Tz1-
Tz28) were synthesized in search of potential anti-diabetic agents. Molecular docking study …

The nuclear receptor PPARγ individually responds to serotonin‐and fatty acid‐metabolites

T Waku, T Shiraki, T Oyama, K Maebara… - The EMBO …, 2010 - embopress.org
The nuclear receptor, peroxisome proliferator‐activated receptor γ (PPARγ), recognizes
various synthetic and endogenous ligands by the ligand‐binding domain. Fatty‐acid …

PPAR agonists: multimodal drugs for the treatment of type-2 diabetes

B Gross, B Staels - Best Practice & Research Clinical Endocrinology & …, 2007 - Elsevier
Patients with type-2 diabetes mellitus (T2DM) are considered to be at particularly high risk
for cardiovascular disease. Over the last decade, the members of the peroxisome proliferator …

[HTML][HTML] Structural basis of the activation of PPARγ by the plasticizer metabolites MEHP and MINCH

A Useini, F Engelberger, G Künze, N Sträter - Environment International, 2023 - Elsevier
Abstract Di-2-ethylhexyl phthalate (DEHP) and its substitute 1, 2-cyclohexane dicarboxylic
acid diisononyl ester (DINCH) are widely used as plasticizers but may have adverse health …

In silico and in vitro analysis of PPAR–α/γ dual agonists: Comparative evaluation of potential phytochemicals with anti-obesity drug orlistat

SK Mandal, BK Kumar, PK Sharma… - Computers in Biology …, 2022 - Elsevier
Obesity is an abnormal fat accumulation disorder in the metabolic syndrome constellation,
and a risk factor for diabetes, cardiovascular disorders, non-alcoholic fatty liver disease …

Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4 (3H)-one derivatives as potential PPARγ and SUR agonists

MK Ibrahim, IH Eissa, MS Alesawy, AM Metwaly… - Bioorganic & medicinal …, 2017 - Elsevier
Peroxisome proliferator-activated receptor gamma (PPARγ) and sulfonylurea receptor
(SUR) play crucial roles in management of type-2 diabetes mellitus. In this study, a series of …

Medicinal chemistry perspective of fused isoxazole derivatives

MA Barmade, PR Murumkar… - Current Topics in …, 2016 - ingentaconnect.com
Nitrogen containing heterocyclic rings with an oxygen atom is considered as one of the best
combination in medicinal chemistry due to their diversified biological activities. Isoxazole, a …