144061-14-3

Usage

Uses

Used in Pharmaceutical Industry:
ETHYL 4-METHYL-2-[3-(TRIFLUOROMETHYL)PHENYL]THIAZOLE-5-CARBOXYLAT is used as a pharmaceutical agent for its antimicrobial properties, contributing to the development of treatments for various infections caused by bacteria and other microorganisms.
Used in Agrochemical Industry:
In the agrochemical sector, ETHYL 4-METHYL-2-[3-(TRIFLUOROMETHYL)PHENYL]THIAZOLE-5-CARBOXYLAT is employed as an antifungal and insecticidal agent, helping to protect crops from fungal diseases and insect pests, thereby enhancing crop yield and quality.

Upstream product

• 53515-17-6 3-(trifluoromethyl)benzothioamide 
• 609-15-4 ethyl 2-chloro-3-oxo-butyrate 
• 53515-17-6 3-trifluoromethyl-thiobenzamide 
• 638-07-3 ethyl (2-chloroaceto)acetate 
• 1801-10-1 3-trifluoromethylbenzamide 
• 368-77-4 3-trifluoromethylbenzonitrile 

Downstream Products

• 668477-94-9 4-methyl-2-[3-(trifluoromethyl)phenyl]thiazole-5-methanol 
• 929693-73-2 ethyl 2-methyl-2-[(4-{[({4-methyl-2-[3-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}carbonyl)amino]methyl}phenyl)oxy]propanoate 
• 144059-85-8 4-methyl-2-[3-(trifluoromethyl)phenyl]-1,3-thiazole-5-carboxylic acid 

Relevant academic research and scientific papers

Synthesis and Evaluation of PPARδAgonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis

We synthesized a directed library of compounds to explore the structure-activity relationships of peroxisome proliferator-activated receptor δ(PPARδ) activation relative to mesenchymal stem cell (MSC) osteogenesis. Our scaffold used para-substituted cinnamic acids as a polar headgroup, a heteroatom and heterocycle core connecting units, and substituted phenyl groups for the lipophilic tail. Compounds were screened for their ability to increase osteogenesis in MSCs, and the most promising were examined for subunit specificity using a quantitative PPAR transactivation assay. Six compounds were selected for in vivo studies in an ovariectomized mouse model of human postmenopausal osteoporosis. Four compounds improved bone density in vivo, with two (12d and 31a) having activity comparable to that of GW0742, a well-studied PPARδ-selective agonist. 31a (2-methyl-4-[N-methyl-N-[5-methylene-4-methyl-2-[4-(trifluoromethyl)phenyl]thiazole]]aminocinnamic acid) had the highest selectivity for PPARδcompared to other subtypes, its selectivity far exceeding that of GW0742. Our results confirm that PPARδis a new drug target for possible treatment of osteoporosis via in situ manipulation of MSCs.

Biphenyl heterocyclic derivatives, their preparation and their use as medicaments (by machine translation)

The present invention relates to a novel biphenyl heterocyclic derivative represented by a general formula (I) and a preparation method thereof and use of a pharmaceutical composition containing the derivative for preparation of a drug for treating diabetes. The biphenyl heterocyclic derivative has extremely excellent hypoglycemic activity in vivo, and excellent in vivo safety and low liver toxicity risk of the compound having such a structure are unexpectedly found, and the novel biphenyl heterocyclic derivative may be used for preventing or treating diabetes.

Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes

The free fatty acid receptor 1 (FFA1/GPR40) has attracted interest as a novel target for the treatment of type 2 diabetes. Several series of FFA1 agonists including TAK-875, the most advanced compound terminated in phase III studies due to concerns about liver toxicity, have been hampered by relatively high molecular weight and lipophilicity. Aiming to develop potent FFA1 agonists with low risk of liver toxicity by decreasing the lipophilicity, the middle phenyl of TAK-875 was replaced by 11 polar five-membered heteroaromatics. Subsequently, systematic exploration of SAR and application of molecular modeling, leads to the identification of compound 44, which was an excellent FFA1 agonist with robustly hypoglycemic effect both in normal and type 2 diabetic mice, low risks of hypoglycemia and liver toxicity even at the twice molar dose of TAK-875. Meanwhile, two important findings were noted. First, the methyl group in our thiazole series occupied a small hydrophobic subpocket which had no interactions with TAK-875. Furthermore, the agonistic activity revealed a good correlation with the dihedral angle between thiazole core and the terminal benzene ring. These results promote the understanding of ligand-binding pocket and might help to design more promising FFA1 agonists.

ANALOGS OF PPARO AND 20-OH-PGE2, AND METHODS OF USING THE SAME

Analogs of PPAR5 and analogs of 20-OH-PGE2, which are PPAR5 agonists and 20-OH-PGE2 antagonists, respectively, and methods of using the same for inducing osteogenesis or chondrogenesis, are disclosed.

HETEROCYCLIC DERIVATIVE AND USE THEREOF

The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.

Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARα agonists. 1. Discovery of a novel series of potent HDLc raising agents

The peroxisome proliferator activated receptors PPARα, PPARγ, and PPARδ are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-density lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARα agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARα agonists. Modification of the selective PPARδ agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARα agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARα and at least 500-fold selectivity versus PPARγ and PPARγ. Compound 25a (GW590735) has been progressed to clinical trials for the treatment of diseases of lipid imbalance.

Thiazolyl-indole derivatives, their manufacture and use as pharmaceutical agents

This invention relates to compounds of the formula wherein one of R6, R7 or R8 is and all enantiomers and pharmaceutically acceptable salts and/or esters thereof as well as pharmaceutical compositions containing such compo