2644-96-4

Upstream product

• 5680-79-5 glycine ethyl ester hydrochloride 
• 122-04-3 4-nitro-benzoyl chloride 
• 616-34-2 methoxycarbonylmethylamine 
• 555-16-8 4-nitrobenzaldehdye 
• 2645-07-0 4-nitrohippuric acid 
• 67-56-1 methanol 

Downstream Products

• 125700-18-7 α-methoxy-N-(4-nitrobenzoyl)glycine methyl ester 
• 125700-19-8 Dimethoxy-(4-nitro-benzoylamino)-acetic acid methyl ester 
• 51769-91-6 1-[N-(4-nitro-benzoyl)-glycyl]-pyrrolidine 
• 139645-87-7 N-(4-nitro-benzoyl)-glycine hydrazide 
• 61-78-9 p-Aminohippuric acid 
• 1268161-49-4 5-chloro-2-(4-nitrophenyl)oxazole-4-carbaldehyde 
• 192758-25-1 3-[methoxycarbonylmethyl-(4-nitro-benzoyl)-amino]-2-diazo-3-oxo-propionic acid methyl ester 
• 5259-86-9 (4-amino-benzoylamino)-acetic acid methyl ester 

Relevant academic research and scientific papers

Dissociation of amides in strongly basic medium of sodium methoxide in dimethyl sulfoxide-methanol mixtures

The dissociation constants of eleven amides have been measured in methanol and its mixtures with dimethyl sulfoxide (10 to 80% v/v) using sodium methoxide as the base. The experimental dissociation constants have been used to construct the H- acidity function as a function of methoxide concentration and composition of the DMSO-MeOH mixture as well as function of methoxide concentration in methanol. Moreover, with the help of construction of acidity function, the functions have been devised for constant sodium methoxide concentrations (0.025, 0.1, and 0.2 mol 1-1) and changing composition of the DMSO-MeOH mixture.

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

Magnetic CuFe2O4nanoparticles: A retrievable catalyst for oxidative amidation of aldehydes with amine hydrochloride salts

The application of magnetic CuFe2O4nanoparticles for the oxidative amidation of aldehydes with amine hydrochloride salts is described. A wide range of amides have been synthesized in good to excellent yields under mild conditions. Chiral amide also synthesized from its corresponding chiral amine salt with retention of the stereochemistry. In particular, the performance of the magnetic separation of the catalyst was very efficient and an alternative to time, solvent and energy-consuming separation procedures. The catalytic activity of the catalyst remains unaltered after five consecutive cycles, making it environmentally benign and widely applicable due to its efficiency, ease of handling and cost effectiveness.

Magnetic CuFe2O4 nanoparticles: A retrievable catalyst for oxidative amidation of aldehydes with amine hydrochloride salts

The application of magnetic CuFe2O4 nanoparticles for the oxidative amidation of aldehydes with amine hydrochloride salts is described. A wide range of amides have been synthesized in good to excellent yields under mild conditions. Chiral amide also synthesized from its corresponding chiral amine salt with retention of the stereochemistry. In particular, the performance of the magnetic separation of the catalyst was very efficient and an alternative to time, solvent and energy-consuming separation procedures. The catalytic activity of the catalyst remains unaltered after five consecutive cycles, making it environmentally benign and widely applicable due to its efficiency, ease of handling and cost effectiveness.

Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein

HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC50 values of 0.21 and 0.17 μΜ, respectively.

Substituent effect on acidity of substituted 2-(4-nitrobenzoylamino)alkanamidesin methanol-dimethyl sulfoxide mixtures

The dissociation constants of substituted 2-(4-nitrobenzoylamino)alkanamides, N-[2-(4-nitrobenzoylamino)aikanoyl]pyrrolidines, and N-alkyl-4-nitrobenzamides have been measured spectrophotometrically in 60 and 80% v/v DMSO. The pKA values of these N-acids are discussed from the point of view of substituents at the acetamide a-carbon atom.

Site selectivity in the Rhodium(II)-catalyzed reaction of α-diazoimides. Ligand and substituent effects

The product distribution obtained from Rh(II)-catalyzed decomposition of α-diazoimides derived from glycine methyl ester has been found to be selectively controlled by the proper choice of catalyst. When the reaction was carried out using perfluorinated l