61954-82-3

Usage

InChI:InChI=1/C9H7BrN2S/c10-8-7(12-9(11)13-8)6-4-2-1-3-5-6/h1-5H,(H2,11,12)

Upstream product

• 2010-06-2 2-Amino-4-phenylthiazole 
• 98-86-2 acetophenone 
• 5039-09-8 2-acetamide-4-phenyl-1,3-thiazole 
• 70-11-1 α-bromoacetophenone 
• 17356-08-0 thiourea 
• 113511-22-1 5-bromo-4-phenyl-thiazol-2-ylamine; hydrobromide 

Downstream Products

• 185335-68-6 1-(5'-bromo-4'-phenylthiazolyl)-3-(2-chloroethyl)urea 
• 1173170-77-8 1,2-bis(2-amino-4-phenylthiazol-5-yl)hydrazine 
• 1391980-01-0 4-phenyl-5-{[4-(trifluoromethyl)phenyl]oxy}-1,3-thiazol-2-amine 
• 1391980-00-9 4-phenyl-5-{[2-(trifluoromethyl)phenyl]oxy}-1,3-thiazol-2-amine 
• 6318-74-7 2-amino-4,5-diphenylthiazole 
• 1391979-65-9 2-[4-(ethylsulfonyl)phenyl]-N-(5-{[4-(methyloxy)phenyl]oxy}-4-phenyl-1,3-thiazol-2-yl)acetamide 
• 1391979-63-7 2-[4-(ethylsulfonyl)phenyl]-N-(4-phenyl-5-{[4-(trifluoromethyl)phenyl]oxy}-1,3-thiazol-2-yl)acetamide 
• 1391979-61-5 N-{5-[(4-chlorophenyl)oxy]-4-phenyl-1,3-thiazol-2-yl}-2-[4-(ethylsulfonyl)phenyl]acetamide 
• 1391979-59-1 2-[4-(ethylsulfonyl)phenyl]-N-(4-phenyl-5-{[2-(trifluoromethyl)phenyl]oxy}-1,3-thiazol-2-yl)acetamide 

Relevant academic research and scientific papers

SUBSTITUTED PROPANAMIDES AS INHIBITORS OF NUCLEASES

The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES

The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

Substituted thiazole derivative and application thereof

The invention provides a compound represented by a general formula (I), or a stereoisomer, pharmaceutically acceptable salt, solvate, hydrate, chemically protective form or prodrug thereof. The compound has an effect of inhibiting adenosine receptor 2a (A2a), and can be used as an antagonist of the adenosine receptor 2a (A2A) for treating tumors.

THIAZOLE MODULATORS OF A3 ADENOSINE RECEPTORS

Modulators of adenosin A3 receptors of formula (I) and procedure for preparing these compounds. Other objectives of the present invention are to provide pharmaceutical compositions comprising an effective amount of these compounds and the use o

Synthesis, biological evaluation and molecular docking studies of thiazole-based pyrrolidinones and isoindolinediones as anticonvulsant agents

A series of new 1-(thiazol-2-yl)pyrrolidin-2-one 5a-m and 2-(thiazol-2-yl)isoindoline-1,3-dione 6a-n derivatives were synthesized and evaluated for anticonvulsant activity. The activity was established in three seizure models: PTZ, picrotoxin and MES. Selected compounds were elected for neurotoxicity by the rotarod test. The most active compound of the series was 1-(4-(naphthalen-2-yl)thiazol-2-yl)pyrrolidin-2-one (5g), showing a PTZ effect dose (ED50) value of 18.4 mg/kg in mice. The median toxic dose (TD50) was 170.2 mg/kg, which provided a protection index (PI = TD50/ED50) of 9.2. A computational study was also carried out, including prediction of pharmacokinetic properties and docking studies. The structural assignments of the newly synthesized compounds were elucidated on the basis of spectroscopic data and single-crystal X-ray crystallography. Graphical Abstract: A series of new thiazole-based pyrrolidinones 5a-m and isoindolinediones 6a-l were synthesized and tested as anticonvulsant. The most active compound was 1-(4-(naphthalen-2-yl)thiazol-2-yl)pyrrolidin-2-one (5g), showing ED50 value 18.4 mg/kg.[Figure not available: see fulltext.]

Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists

A novel series of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as RORγt inverse agonists was discovered. Binding mode analysis of a RORγt partial agonist (2c) revealed by co-crystal structure in RORγt LBD suggests that the inverse agonists do not directly interfere with the interaction between H12 and the RORγt LBD. Detailed SAR exploration led to identification of potent RORγt inverse agonists such as 3m with a pIC50 of 8.0. Selected compounds in the series showed reasonable activity in Th17 cell differentiation assay as well as low intrinsic clearance in mouse liver microsomes.

2-amino-4-arylthiazole derivatives as anti-giardial agents: Synthesis, biological evaluation and QSAR studies

A series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch's modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50= 0.39 μM) and 6b (IC50= 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors

Novel series of N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides were discovered as potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitors. SAR studies of the RORγt HTS hit 6a led to identification of thiazole ketone amide 8h and thiophene ketone amide 9g with high binding affinity and inhibitory activity of Th17 cell differentiation. Compound 8h showed in vivo efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models via oral administration.

COMPOUNDS USEFUL AS RETINOID-RELATED ORPHAN RECEPTOR GAMMA MODULATORS

Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators of Formula (I) and their use in the treatment of diseases mediated by RORγ, wherein the radicals have the meanings as defined in the invention.