Multitargeted bioactive ligands for PPARs discovered in the last decade

Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists: Effects on the affinity and selectivity towards PPARβ/δ

(2016) Åsmund Kaupang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of novel Y-shaped barbituric acid derivatives as PPARγ activators

(2016) Vaibhav A. Dixit et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PPAR-pan activation induces hepatic oxidative stress and lipidomic remodelling

(2016) Zsuzsanna Ament et al.   FREE RADICAL BIOLOGY AND MEDICINE

Pioglitazone Inhibits the Development of Hyperalgesia and Sensitization of Spinal Nociresponsive Neurons in Type 2 Diabetes

(2016) Ryan B. Griggs et al.   JOURNAL OF PAIN

L312, a novel PPARγ ligand with potent anti-diabetic activity by selective regulation

(2015) Xinni Xie et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Identification of dual PPARα/γ agonists and their effects on lipid metabolism

(2015) Quanqing Gao et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists

(2015) Hao Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel 2,7-Substituted (S)-1,2,3,4-Tetrahydroisoquinoline-3-carboxylic Acids: Peroxisome Proliferator-Activated Receptor γ Partial Agonists with Protein–Tyrosine Phosphatase 1B Inhibition

(2015) Kazuya Otake et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Pharmacokinetic Interaction Between Amlodipine and Lobeglitazone, a Novel Peroxisome Proliferator–activated Receptor-γ Agonist, in Healthy Subjects

(2015) Choon OK Kim et al.   CLINICAL THERAPEUTICS

Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618

(2015) Åsmund Kaupang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats

(2015) Jong-Hwa Lee et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Silymarin Constituents Enhance ABCA1 Expression in THP-1 Macrophages

(2015) Limei Wang et al.   MOLECULES

PPAR-αAgonist Fenofibrate Decreased Serum Irisin Levels in Type 2 Diabetes Patients with Hypertriglyceridemia

(2015) Xiaomeng Feng et al.   PPAR Research

Observational Study of Effects of Saroglitazar on Glycaemic and Lipid Parameters on Indian Patients with Type 2 Diabetes

(2015) Sanjay Chatterjee et al.   Scientific Reports

Identification of a novel selective agonist of PPARγ with no promotion of adipogenesis and less inhibition of osteoblastogenesis

(2015) Chang Liu et al.   Scientific Reports

Characterisation of Pain Responses in the High Fat Diet/Streptozotocin Model of Diabetes and the Analgesic Effects of Antidiabetic Treatments

(2015) Frederika Maria Byrne et al.   Journal of Diabetes Research

Saroglitazar for the treatment of hypertriglyceridemia in patients with type 2 diabetes: current evidence

(2015) Sosale Aravind Sosale et al.   Diabetes Metabolic Syndrome and Obesity-Targets and Therapy

Structure-Based Virtual Screening and Discovery of New PPARδ/γ Dual Agonist and PPARδ and γ Agonists

(2015) Vinicius G. Maltarollo et al.   PLoS One

The First Approved Agent in the Glitazar’s Class: Saroglitazar

(2014) Ritesh Agrawal   CURRENT DRUG TARGETS

The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma–associated adverse cardiac effects

(2014) Rémy Hanf et al.   Diabetes & Vascular Disease Research

LT175 Is a Novel PPARα/γ Ligand with Potent Insulin-sensitizing Effects and Reduced Adipogenic Properties

(2014) Federica Gilardi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Isosilybin A from Milk Thistle Seeds as an Agonist of Peroxisome Proliferator-Activated Receptor Gamma

(2014) Eva-Maria Pferschy-Wenzig et al.   JOURNAL OF NATURAL PRODUCTS

Insulin Sensitization by a Novel Partial Peroxisome Proliferator-Activated Receptor γ Agonist With Protein Tyrosine Phosphatase 1B Inhibitory Activity in Experimental Osteoporotic Rats

(2014) Masahiro Kubo et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Novel PPAR Pan Agonist, ZBH Ameliorates Hyperlipidemia and Insulin Resistance in High Fat Diet Induced Hyperlipidemic Hamster

(2014) Wei Chen et al.   PLoS One

Efficacy and Safety of Lobeglitazone Monotherapy in Patients with Type 2 Diabetes Mellitus over 24-Weeks: A Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo Controlled Trial

(2014) Sin Gon Kim et al.   PLoS One

Carcinogenicity study of CKD-501, a novel dual peroxisome proliferator-activated receptors α and γ agonist, following oral administration to Sprague Dawley rats for 94–101weeks

(2014) Hee Su Lee et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Protopanaxatriol, a novel PPARγ antagonist from Panax ginseng, alleviates steatosis in mice

(2014) Yu Zhang et al.   Scientific Reports

Design and synthesis of a series of α-benzyl phenylpropanoic acid-type peroxisome proliferator-activated receptor (PPAR) gamma partial agonists with improved aqueous solubility

(2013) Masao Ohashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and evaluation of 2,3-dinorprostaglandins: Dinor-PGD1 and 13-epi-dinor-PGD1 are peroxisome proliferator-activated receptor α/γ dual agonists

(2013) Ayato Sato et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

γ-Mangostin fromGarcinia MangostanaPericarps as a Dual Agonist That Activates Both PPARα and PPARδ

(2013) Nobuyasu MATSUURA et al.   BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY

Synthesis and Structure–Activity Relationships of Novel Zwitterionic Compounds as Peroxisome Proliferator Activated Receptor α/γ Dual Agonists with Improved Physicochemical Properties

(2013) Yoshihiro Shibata et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Pharmacokinetics, Safety, and Tolerability of Saroglitazar (ZYH1), a Predominantly PPARα Agonist with Moderate PPARγ Agonist Activity in Healthy Human Subjects

(2013) Rajendra H. Jani et al.   CLINICAL DRUG INVESTIGATION

Dual Peroxisome Proliferator-Activated Receptor  /  Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in Abdominally Obese Subjects

(2013) B. Cariou et al.   DIABETES CARE

Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis

(2013) Bart Staels et al.   HEPATOLOGY

Potent Anti-Diabetic Effects of MHY908, a Newly Synthesized PPAR α/γ Dual Agonist in db/db Mice

(2013) Min Hi Park et al.   PLoS One

Pseudoginsenoside F11, a Novel Partial PPARγAgonist, Promotes Adiponectin Oligomerization and Secretion in 3T3-L1 Adipocytes

(2013) Guoyu Wu et al.   PPAR Research

Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1)

(2012) Yoshihiro Shibata et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, development and evaluation of novel dual PPARδ/PPARγ agonists

(2012) Symon Gathiaka et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-γ/δ agonists

(2012) Hyo Jin Gim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo

(2012) Jungyeob Ham et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Three-in-one agonists for PPAR-α, PPAR-γ, and PPAR-δ from traditional Chinese medicine

(2012) Kuan-Chung Chen et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

In VitroandIn VivoCharacterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist

(2012) B. K. He et al.   PPAR Research

Sulfonylthiadiazoles with an Unusual Binding Mode as Partial Dual Peroxisome Proliferator-Activated Receptor (PPAR) γ/δ Agonists with High Potency and in vivo Efficacy

(2011) Stefanie Keil et al.   ChemMedChem

Activation of peroxisome proliferator-activated receptor-alpha stimulates both differentiation and fatty acid oxidation in adipocytes

(2011) Tsuyoshi Goto et al.   JOURNAL OF LIPID RESEARCH

Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ-selective partial agonists by disruption of molecular planarity/symmetry

(2010) Jun-ichi Kasuga et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Effect of structurally constrained oxime–ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists

(2010) Pankaj Makadia et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A stereo-controlled synthesis of 2,4-dimethyl-4-hydroxy-16-phenylhexadecanoic acid 1,4-lactone and its PPAR activities

(2010) Jaeyoung Ko et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cevoglitazar, a Novel Peroxisome Proliferator-Activated Receptor-α/γ Dual Agonist, Potently Reduces Food Intake and Body Weight in Obese Mice and Cynomolgus Monkeys

(2010) Hong Chen et al.   ENDOCRINOLOGY

PAM-1616, a selective peroxisome proliferator-activated receptor γ modulator with preserved anti-diabetic efficacy and reduced adverse effects

(2010) Mi-Kyung Kim et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Identification and Characterization of 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a Selective and Irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) Antagonist

(2010) Barry G. Shearer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Structure−Activity Relationship Studies of Novel 2,4,6-Trisubstituted-5-pyrimidinecarboxylic Acids as Peroxisome Proliferator-Activated Receptor γ (PPARγ) Partial Agonists with Comparable Antidiabetic Efficacy to Rosiglitazone

(2010) Shigeki Seto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Structural Analysis of Phenylpropanoic Acid-Type PPARγ-Selective Agonists: Discovery of Reversed Stereochemistry−Activity Relationship

(2010) Masao Ohashi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of novel PPARα/γ dual agonists as potential drugs for the treatment of the metabolic syndrome and diabetes type II designed using a new de novo design programprotobuild

(2010) Yushma Bhurruth-Alcor et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Adaptability and selectivity of human peroxisome proliferator-activated receptor (PPAR) pan agonists revealed from crystal structures

(2009) Takuji Oyama et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PAR-1622 is a selective peroxisome proliferator-activated receptor γ partial activator with preserved antidiabetic efficacy and broader safety profile for fluid retention

(2009) Mi-Kyung Kim et al.   ARCHIVES OF PHARMACAL RESEARCH

Antagonist of peroxisome proliferator-activated receptor γ induces cerebellar amyloid-β levels and motor dysfunction in APP/PS1 transgenic mice

(2009) Jing Du et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A pan-PPAR ligand induces hepatic fatty acid oxidation in PPARα−/− mice possibly through PGC-1 mediated PPARδ coactivation

(2009) Therese H. Røst et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Identification of a PPARδ agonist with partial agonistic activity on PPARγ

(2009) Richard V. Connors et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and structure–activity relationships of azole acids as novel, potent dual PPAR α/γ agonists

(2009) Hao Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists

(2009) Jun-ichi Kasuga et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel phospholipid analogues of pan-PPAR activator tetradecylthioacetic acid are more PPARα selective

(2009) Yushma Bhurruth-Alcor et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The dual PPARα/γ agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice

(2009) JWA Van Der Hoorn et al.   BRITISH JOURNAL OF PHARMACOLOGY

P633H, a novel dual agonist at peroxisome proliferator-activated receptors α and γ, with different anti-diabetic effects indb/dband KK-Aymice

(2009) Wei Chen et al.   BRITISH JOURNAL OF PHARMACOLOGY

PPAR γ partial agonist, KR-62776, inhibits adipocyte differentiation via activation of ERK

(2009) J. Kim et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Effects of cevoglitazar, a dual PPARα/γ agonist, on ectopic fat deposition in fatty Zucker rats

(2009)   DIABETES OBESITY & METABOLISM

Improved insulin sensitivity and islet function after PPARδ activation in diabetic db/db mice

(2009) Maria Sörhede Winzell et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic Acid (MK-0533): A Novel Selective Peroxisome Proliferator-Activated Receptor γ Modulator for the Treatment of Type 2 Diabetes Mellitus with a Reduced Potential to Increase Plasma and Extracellular Fluid Volume

(2009) John J. Acton et al.   JOURNAL OF MEDICINAL CHEMISTRY

7-Hydroxy-benzopyran-4-one Derivatives: A Novel Pharmacophore of Peroxisome Proliferator-Activated Receptor α and -γ (PPARα and γ) Dual Agonists

(2009) Azadeh Matin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effect of the dual peroxisome proliferator-activated receptor-α/γ agonist aleglitazar on risk of cardiovascular disease in patients with type 2 diabetes (SYNCHRONY): a phase II, randomised, dose-ranging study

(2009) Robert R Henry et al.   LANCET

Design and Synthesis of Thiazolidinedione Derivates as Selective PPARγ Modulators

(2009) Xiangyang Sha et al.   Letters in Drug Design & Discovery

Understanding and Controlling the Formation of an Impurity during the Development of Muraglitazar, a PPAR Dual Agonist

(2009) Qingmei Ye et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Regulation of advanced glycation end product (AGE)-receptor (RAGE) system by PPAR-gamma agonists and its implication in cardiovascular disease

(2009) Sho-ichi Yamagishi et al.   PHARMACOLOGICAL RESEARCH

Interaction Models of a Series of Oxadiazole-Substituted α-Isopropoxy Phenylpropanoic Acids Against PPARα and PPARγ: Molecular Modeling and Comparative Molecular Similarity Indices Analysis Studies

(2009) Feng Cheng et al.   PROTEIN AND PEPTIDE LETTERS

MBX-102/JNJ39659100, a Novel Non-TZD Selective Partial PPAR- Agonist Lowers Triglyceride Independently of PPAR- Activation

(2009) Apurva Chandalia et al.   PPAR Research

Design and synthesis of novel oxazole containing 1,3-Dioxane-2-carboxylic acid derivatives as PPAR α/γ dual agonists

(2008) Harikishore Pingali et al.   BIOORGANIC & MEDICINAL CHEMISTRY

SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail

(2008) Jun-ichi Kasuga et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part

(2008) Jun-ichi Kasuga et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of a series of benzopyran derivatives as PPAR α/γ agonists

(2008) Juanhong Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Oregano: A Source for Peroxisome Proliferator-Activated Receptor γ Antagonists

(2008) Monika Mueller et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Design, Synthesis, and Biological Evaluation of Novel Constrainedmeta-Substituted Phenyl Propanoic Acids as Peroxisome Proliferator-Activated Receptor α and γ Dual Agonists

(2008) Young-Ger Suh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel PPAR Ligands by a Virtual Screening Approach Based on Pharmacophore Modeling, 3D Shape, and Electrostatic Similarity Screening

(2008) Patrick Markt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular mechanics and molecular orbital simulations on specific interactions between peroxisome proliferator-activated receptor PPARα and plasticizer

(2008) Tomohiko Nakagawa et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Identification of a novel agonist of peroxisome proliferator-activated receptors α and γ that may contribute to the anti-diabetic activity of guggulipid in Lepob/Lepob mice

(2008) Claire L. Cornick et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Synthesis of a Novel Series of 8-HETE Analogs and their Biological Evaluation Towards the PPAR Nuclear Receptors

(2008) Melanie Liutkus et al.   Letters in Drug Design & Discovery

Tesaglitazar, a dual peroxisome proliferator-activated receptor α/γ agonist, improves apolipoprotein levels in non-diabetic subjects with insulin resistance

(2007) Herbert Schuster et al.   ATHEROSCLEROSIS

Increase in weight induced by muraglitazar, a dual PPARα/γ agonist, in db/db mice: adipogenesis/or oedema?

(2007) S Mittra et al.   BRITISH JOURNAL OF PHARMACOLOGY

Identification and Characterization of a Selective Peroxisome Proliferator-Activated Receptor β/δ (NR1C2) Antagonist

(2007) Barry G. Shearer et al.   MOLECULAR ENDOCRINOLOGY