5259-86-9

Usage

InChI:InChI=1/C10H12N2O3/c1-15-9(13)6-12-10(14)7-2-4-8(11)5-3-7/h2-5H,6,11H2,1H3,(H,12,14)

Upstream product

• 2644-96-4 2-(4-nitrobenzamido)acetic acid methyl ester 
• 122-04-3 4-nitro-benzoyl chloride 
• 2645-07-0 4-nitrohippuric acid 
• 5680-79-5 glycine ethyl ester hydrochloride 
• 540-37-4 p-aminoiodobenzene 
• 13939-06-5 molybdenum hexacarbonyl 

Downstream Products

• 67726-12-9 N-{4-[(2-oxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glycine methyl ester 
• 67726-17-4 N-{4-[(2-thioxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glycine methyl ester 
• 67726-23-2 N-{4-[(2-thioxo-benzothiazol-3-ylmethyl)-amino]-benzoyl}-glycine methyl ester 
• 79023-33-9 p-<(p-hydroxybenzylidene) amino> hippuric acid methyl ester 
• 79023-22-6 p-<(p-methoxybenzylidene)amino>hippuric acid methyl ester 
• 79023-29-3 p-<(o-hydroxybenzylidene) amino> hippuric acid methyl ester 
• 1043345-15-8 C₂₄H₁₉F₃N₂O₄ 

Relevant academic research and scientific papers

Searching new structural scaffolds for BRAF inhibitors. An integrative study using theoretical and experimental techniques

The identification of the V600E activating mutation in the protein kinase BRAF in around 50% of melanoma patients has driven the development of highly potent small inhibitors (BRAFi) of the mutated protein. To date, Dabrafenib and Vemurafenib, two specifi

Synthesis and Evaluation of N-Phenylpyrrolamides as DNA Gyrase B Inhibitors

ATP-competitive inhibitors of DNA gyrase and topoisomerase IV are among the most interesting classes of antibacterial drugs that are unrepresented in the antibacterial pipeline. We developed 32 new N-phenylpyrrolamides and evaluated them against DNA gyrase and topoisomerase IV from E. coli and Staphylococcus aureus. Antibacterial activities were studied against Gram-positive and Gram-negative bacterial strains. The most potent compound displayed an IC50 of 47 nm against E. coli DNA gyrase, and a minimum inhibitory concentration (MIC) of 12.5 μm against the Gram-positive Enterococcus faecalis. Some compounds displayed good antibacterial activities against an efflux-pump-deficient E. coli strain (MIC=6.25 μm) and against wild-type E. coli in the presence of efflux pump inhibitor PAβN (MIC=3.13 μm). Here we describe new findings regarding the structure–activity relationships of N-phenylpyrrolamide DNA gyrase B inhibitors and investigate the factors that are important for the antibacterial activity of this class of compounds.

Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2

EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing substituted diaryl urea or glycine methyl ester moiety were designed and identified as EGFR and VEGFR-2 dual inhibitors. Compounds 19i, 19j and 19l exhibited the most potent inhibitory activities against EGFR (IC50?=?1?nM, 78?nM and 51?nM, respectively) and VEGFR-2 (IC50?=?79?nM, 14?nM and 14?nM, respectively), they showed good antiproliferative activities as well. Molecular docking established the interaction of 19i with the DFG-out conformation of VEGFR-2, suggesting that they might be type II kinase inhibitors.

N-Phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATP Competitive DNA Gyrase B Inhibitors: Design, Synthesis, and Evaluation

Bacterial DNA gyrase is a well-known and validated target in the design of antibacterial drugs. However, inhibitors of its ATP binding subunit, DNA gyrase B (GyrB), have so far not reached clinical use. In the present study, three different series of N-ph

Expedient carbonylation of aryl halides in aqueous or neat condition

An expedient and versatile, microwave-assisted procedure for the carbonylation of aryl halides with boronic acids, alcohols or amines in water or under neat conditions has been developed. The reaction is catalyzed by fluorous, oxime-based palladacycle 1 that shows an excellent recyclable property and low levels of Pd leaching. To demonstrate the usefulness of the protocol, we applied it to the preparation of compounds of pharmaceutical interest, including a precursor of the reverse transcriptase inhibitor, niacin, benzocaine and butamben.

THIAZOLE DERIVATIVES AND USE THEREOF

The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.