4815-43-4

Upstream product

• 14442-50-3 2-cyano-3,4-diphenyl-crotonic acid ethyl ester 
• 71-43-2 benzene 
• 105-56-6 ethyl 2-cyanoacetate 
• 451-40-1 phenyl benzyl ketone 
• 103-80-0 phenylacetyl chloride 

Downstream Products

• 538326-96-4 N-[3-(biphenyl-4-carbonyl)-4,5-diphenylthiophen-2-yl]-2,2,2-trifluoroacetamide 
• 538326-97-5 N-[3-(naphthalene-2-carbonyl)-4,5-diphenylthiophen-2-yl]-2,2,2-trifluoroacetamide 
• 538326-94-2 N-[3-(3-chlorobenzoyl)-4,5-diphenylthiophen-2-yl]-2,2,2-trifluoroacetamide 
• 538326-95-3 N-[3-(4-chlorobenzoyl)-4,5-diphenylthiophen-2-yl]-2,2,2-trifluoroacetamide 
• 538326-60-2 N-(3-benzoyl-4,5-diphenylthiophen-2-yl)acetamide 
• 538326-91-9 N-(4,5-diphenylthiophen-2-yl)-2,2,2-trifluoroacetamide 
• 538326-59-9 N-(4,5-diphenylthiophen-2-yl)acetamide 

Relevant academic research and scientific papers

Substituted 2-Aminothiopen-derivatives: A potential new class of GluR6-Antagonists

In the course of search for new therapeutic agents against epilepsy new inhibitors for the kainate receptor subtypes GluR5 and GluR6 were synthesized. We were able to synthesize new substituted thieno[2,3-d]pyrimidines 3a,b, 4a,b, 5a,b as well as thiophene-3-carboxamides 2a-d and a multitude of substituted 4-methyl-5-phenylthiophene-3-carboxylic acids. All compounds described herein were tested for their antagonistic effect towards the kainate receptor subtypes GluR5 and GluR6. The highest activity was observed for ethyl 2-amino-4-methyl-5-phenylthiophene-3-carboxylate 1c with an IC50 = 0.75 μM at the GluR6 receptor.

2-Amino-3-benzoylthiophene allosteric enhancers of A1, adenosine agonist binding: New 3, 4-, and 5-modifications

2-Amino-3-aroylthiophenes are agonist allosteric enhancers (AE) at the A1, adenosine receptor (A1AR). Here we report the syntheses of three kinds of novel 2-aminothiophenes and assays of their AE activity at the human A1AR (hA1AR), namely, (1) 2-amino-4,5-diphenylthiophene-3-carboxylates, 3a-h, (2) 2-amino-3-benzoyl-4,5-diphenylthiophenes, 7a-p, and (3) 2-amino-5-bromo-3-benzoyl-4-phenylthiophenes, 10a-h. An in vitro assay employing the A1AR agonist [125I]ABA and membranes from CHO-K1 cells stably expressing the hA1AR measured an index of AE activity, the ability of a candidate AE to stabilize the agonist-A1AR-G protein ternary complex, scored as the percentage of ternary complex remaining after 10 min of dissociation initiated by CPX and GTPγS. The AE activity score of 2-amino-4,5-dimethyl-3-(3-trifluoromethylbenzoyl)thiophene (PD 81,723), which was 19%, served as a standard for comparison. Two 3-carboxythiophene 3-trifluoromethylbenzyl esters, 3d (49%) and 3f (63%), had substantial AE activity. The 3-(1-naphthoyl) substituent of 7e (52%) also supported AE activity. Compounds in series 3 tended to be more potent, 10a and 10c having scores of 91 and 80%, respectively. The activity of 2-amino-5-bromo-3-ethoxycarbonyl-4-(3-nitrophenyl)thiophene, 10h (26%), is an exception to the rule that a 3-ethoxycarbonyl substituent cannot support AE activity.