636589-63-4

Upstream product

• 32281-01-9 4-mercapto-2-methylphenol 
• 317318-97-1 5-(chloromethyl)-4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazole 
• 317318-96-0 [4-methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-methanol 
• 72505-21-6 4-trifluoromethylbenzthioamide 
• 439134-78-8 5-(bromomethyl)-4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazole 
• 95-48-7 ortho-cresol 
• 3774-53-6 2-methyl-4-thiocyanato-phenol 
• 60577-30-2 4-iodo-2-methyl-phenol 
• 2362-12-1 4-Bromo-2-methylphenol 

Downstream Products

• 317318-69-7 methyl [2-methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-yl]methyl]sulfanyl]peroxy]acetate 
• 1268500-86-2 ethyl 2-methyl-2-{2-methyl-4-[(4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-yl)methylthio]phenoxy}propanoate 
• 1268500-84-0 ethyl 2-{2-methyl-4-[(4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-yl)methylthio]phenoxy}propanoate 
• 1268500-53-3 2-{2-methyl-4-[(4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-yl)methylthio]phenoxy}propanoic acid 
• 1026868-55-2 2-methyl-2-{2-methyl-4-[(4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-yl)methylthio]phenoxy}propanoic acid 
• 1383479-82-0 C₃₆H₄₀F₃NO₃S₂ 
• 591775-42-7 2-(2-methyl-4-(1-(4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)-2-phenylethylthio)phenoxy)acetic acid 
• 1383479-80-8 C₃₂H₃₄F₃NOS₂ 

Relevant academic research and scientific papers

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

We have discovered and demonstrated the in vitro and in vivo PPARδ-selective activity of novel Y-shaped agonists. These compounds activated hPPARδ with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the mos

Synthesis, biological evaluation and molecular modeling of GW 501516 analogues

Eleven analogues of GW 501516 (1) were prepared and subjected to biological testing in a semi-high throughput human skeletal muscle cell assay. The assay testing indicated that all analogues elicited oxidation of oleic acid. Among the most potent agonists, 2e (2-{2-ethyl-4-[(4-methyl-2-(4-trifluoromethylphenyl) thiazol-5-yl)methylthio]phenoxy}-2-methylpropanoic acid), was also subjected to a luciferase-based transfection assay, which showed that this compound is a potent agonist against PPARδ and a moderate agonist against PPARα. Docking of compound 2e into PPARδ revealed that it occupied the agonist binding site and exhibited key hydrogen bonding interactions with His323, His449, and Tyr473. Eleven GW 501516 analogues were prepared and subjected to human skeletal muscle cells. The assay testing indicated that all analogues elicited oxidation of oleic acid. One of the analogues displayed dual agonist effects against both PPARα and PPARδ. Copyright

THIAZOLE COMPOUND (AS PPARδ) LIGAND AND PHARMACEUTICAL, COSMETIC AND HEALTH FOOD COMPRISED THEREOF

The present invention relates to a thiazole compound as a peroxisome proliferator activated receptor δ (PPARδ) activator or pharmaceutically acceptable salts thereof, and a pharmaceutical composition, a functional cosmetic composition, a health food, health beverages, a food additive and animal feeds containing the same.

PROCESS FOR PREPARING LIGANDS OF PPARDELTA AND THE INTERMEDIATE COMPOUNDS FOR PREPARING THE SAME

The present invention provides a process for preparing thiazole derivatives of formula (I), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPAR δ ), and also provides compounds of formula (II), (IV), (X), (XI) and (XII), intermediate compounds for preparation of the above compounds of formula (I).

A highly efficient synthesis of antiobestic ligand GW501516 for the peroxisome proliferator-activated receptor δ through in situ protection of the phenol group by reaction with a Grignard reagent

A new synthesis of an agonist for the peroxisome proliferator-activated receptor δ (PPARδ) GW501516 as a potential antiobesity drug is described. The synthetic route involves the in situ protection of the phenol group with a Grignard reagent and a regio-controlled one-pot reaction for the formation of a sulfide bond as the key step. Starting from commercially available 4-iodo-2-methylphenol, this approach affords GW501516 with an overall yield of 87%.

PROCESS FOR PREPARING THIAZOLE DERIVATIVE AND THE INTERMEDIATE COMPOUNDS FOR PREPARING THE SAME

The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPARδ), and also provides processes for compounds of formula (VI), (VII)

A Short and Efficient Synthesis of the Pharmacological Research Tool GW501516 for the Peroxisome Proliferator-Activated Receptor δ

The most potent and selective peroxisome proliferator-activated receptor δ (PPARδ) agonist GW501516 (1) was synthesized in 4 steps and 78% overall yield starting from o-cresol by using a one-pot regiocontrolled dialkylation of mercaptophenol 5 as the key