36977-69-2

Upstream product

• 74457-62-8 N-phenyl 3-benzoyl-3-bromopropionamide 
• 71-43-2 benzene 
• 62-53-3 aniline 
• 117201-53-3 (E)-4-Oxo-4-phenyl-but-2-enoyl chloride 
• 17812-07-6 Benzoylacrylic acid 
• 51241-21-5 C₁₀H₇ClO₂ 
• 53515-22-3 3-bromo-4-oxo-4-phenylbutanoic acid 
• 136163-24-1 N-phenylmaleisoimidium perchlorate 

Downstream Products

• 1220094-63-2 (RS)-4-oxo-N,4-diphenyl-2-(1-piperidinyl)butyramide 
• 1220094-70-1 (RS)-4-phenyl-4-oxo-N-phenyl-2-(4-morpholinyl)butyramide 
• 1612766-15-0 C₂₃H₂₂N₂O₂ 

Relevant academic research and scientific papers

(E)-4-Aryl-4-oxo-2-butenoic acid amides, chalcone-aroylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization

Antiproliferative activity of twenty-nine (E)-4-aryl-4-oxo-2-butenoic acid amides against three human tumor cell lines (HeLa, FemX, and K562) is reported. Compounds showed antiproliferative activity in one-digit micromolar to submicromolar concentrations.

4-Aryl-4-oxo-N-phenyl-2-aminylbutyramides as acetyl- and butyrylcholinesterase inhibitors. Preparation, anticholinesterase activity, docking study, and 3D structure-activity relationship based on molecular interaction fields

Synthesis and anticholinesterase activity of 4-aryl-4-oxo-N-phenyl-2-aminylbutyramides, novel class of reversible, moderately potent cholinesterase inhibitors, are reported. Simple substituent variation on aroyl moiety changes anti-AChE activity for two orders of magnitude; also substitution and type of hetero(ali)cycle in position 2 of butanoic moiety govern AChE/BChE selectivity. The most potent compounds showed mixed-type inhibition, indicating their binding to free enzyme and enzyme-substrate complex. Alignment-independent 3D QSAR study on reported compounds, and compounds having similar potencies obtained from the literature, confirmed that alkyl substitution on aroyl moiety of molecules is requisite for inhibition activity. The presence of hydrophobic moiety at close distance from hydrogen bond acceptor has favorable influence on inhibition potency. Docking studies show that compounds probably bind in the middle of the AChE active site gorge, but are buried deeper inside BChE active site gorge, as a consequence of larger BChE gorge void.

SYNTHESIS AND SOME REACTIONS OF N-ARYLMALEISOIMIDIUM PERCHLORATES

N-Arylmaleisoimidium perchlorates (1a and b) were prepared by the action of acetic anhydride and perchlorid acid on the N-arylmaleamic acids (2a and b).Compound 1b reacted with amines via ring-opening to give N,N-disubstituted maleamides (4a-c), while the reaction of 1a with secondary amines gave N-phenylmaleimide (6).The reaction of 1a and b with aromatic hydrocarbons in the presence of anhydrous aluminium chloride gave good yields of trans-β-aroyl-N-arylacrylamides (7a-h).The reactions of some of the latter compounds with amines and phenylhydrazine are also discussed.

AN ALTERNATIVE ROUTE TO 4-BENZOYL-2-AZETIDINONES

Cyclodehydrohalogenation by terminal N1-C4 bond formation affords N-aryl-4-benzoyl-2-azetidinones from 3-benzoyl-3-bromopropionanilides in an unequivocal annelation process.

Substituted benzoylacrylanilides

Novel substituted benzoylacrylanilides are prepared by reacting a substituted benzoylacrylic acid with a substituted aniline in the presence of a coupling agent. These acrylanilides have significant anticoccidial activity.