88744-17-6

Upstream product

• 13433-00-6 diethyl aminomalonate hydrochloride 
• 103-80-0 phenylacetyl chloride 
• 6829-40-9 aminomalonic acid diethyl ester 

Downstream Products

• 221646-21-5 2-(2-acetoxy-3-tert-butoxycarbonyl-benzyl)-2-phenylacetylamino-malonic acid diethyl ester 
• 507268-57-7 diethyl 2-(4-methoxy-1H-indol-3-ylmethyl)-2-phenylacetylaminomalonate 
• 252288-57-6 4-(N-tert-Butyloxycarbonyl)amino-N-phenylacetyltryptophan 
• 319921-63-6 3-(4-tert-butoxycarbonylamino-1H-indol-3-yl)-2-phenylacetylamino-propionic acid 
• 319921-01-2 Bis(allyl) [4-(N-tert-butyloxycarbonyl)amino-1H-indol-3yl]methylphenylacetamidomalonate 
• 319921-42-1 (R)-[2-(4-Amino-1H-indol-3-yl)-1-(hydroxymethyl)ethyl]phenylacetamide 
• 319921-38-5 (R)-4-Amino-N-phenylacetyltryptophan methyl ester 
• 252289-10-4 (R)-4-(N-tert-Butyloxycarbonyl)amino-N-phenylacetyltryptophan methyl ester 
• 319921-46-5 (R,R)-2-{4-[1-(Phenylmethyloxycarbonyl)ethylamino]-1H-indol-3-yl}-1-(hydroxymethyl)ethylphenylacetamide 
• 872825-04-2 5-ethoxy-2-benzyl-oxazole-4-carboxylic acid 
• 872806-18-3 2-benzyl-5-chloro-oxazole-4-carboxylic acid ethyl ester 
• 855405-27-5 2-benzyl-5-chloro-oxazole-4-carboxylic acid 
• 184536-35-4 N-(4-hydroxy-2-oxo-1,2-dihydro-quinolin-3-yl)-2-phenyl-acetamide 
• 221646-22-6 2-(3-carboxy-2-hydroxy-benzyl)-2-phenylacetylamino-malonic acid 

Relevant academic research and scientific papers

Exploring the 7-oxo-thiazolo[5,4-d]pyrimidine core for the design of new human adenosine A3 receptor antagonists. Synthesis, molecular modeling studies and pharmacological evaluation

A new series of 5-methyl-thiazolo[5,4-d]pyrimidine-7-ones bearing different substituents at position 2 (aryl, heteroaryl and arylamino groups) was synthesized and evaluated in radioligand binding assays to determine their affinities at the human (h) A1, A2A, and A3 adenosine receptors (ARs). Efficacy at the hA2B and antagonism of selected ligands at the hA3 were also assessed through cAMP experiments. Some of the new derivatives exhibited good to high hA3AR affinity and selectivity versus all the other AR subtypes. Compound 2-(4-chlorophenyl)-5-methyl-thiazolo[5,4-d]pyrimidine-7-one 4 was found to be the most potent and selective ligand of the series (Ki hA3 Combining double low line 18 nM). Molecular docking studies of the reported derivatives were carried out to depict their hypothetical binding mode in our hA3 receptor model.

Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors

Human rhinovirus 3C protease (HRV 3Cpro) is known to be a promising target for development of therapeutic agents against the common cold because of the importance of the protease in viral replication as well as its expression in a large number of serotypes. To explore non-peptidic inhibitors of HRV 3Cpro, a series of novel heteroaromatic esters was synthesized and evaluated for inhibitory activity against HRV 3Cpro, to determine the structure-activity relationships. The most potent inhibitor, 7, with a 5-bromopyridinyl group, had an IC50 value of 80 nM. In addition, the binding mode of a novel analog, 19, with the 4-hydroxyquinolinone moiety, was explored by molecular docking, suggesting a new interaction in the S1 pocket.

Total synthesis of the cyclic peptide Argyrin B

The details of the total synthesis of Argyrin B, a natural product with immunosuppressive properties, are reported below. The two most unusual amino acid residues of this cyclic peptide are 4-methoxytryptophan and dehydroalanine, which were obtained by mo

4-hydroxy-2-quinolones. 31. 3-amino-1R-2-oxo-4-hydroxyquinolines and their acyl derivatives

An alternative method has been developed for preparing and studying the antioxidant activity of 3-acylamino-2-oxo-4-hydroxyquinolones. Results are presented from an investigation of the antithyroid and antimicrobial action of the intermediate 2-oxo-3-(1-pyridinio)quinolin-4-olates and the 3-amino-2-oxo-4-hydroxyquinolines. 1997 Plenum Publishing Corporation.