72336-16-4Relevant academic research and scientific papers
Carboxyesterase polypeptides for amide coupling
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Page/Page column 63-64; 68-72; 79-81, (2021/05/28)
The present invention provides engineered carboxyesterase enzymes having improved properties as compared to a naturally occurring wild-type carboxyesterase enzymes, as well as polynucleotides encoding the engineered carboxyesterase enzymes, host cells capable of expressing the engineered carboxyesterase enzymes, and methods of using the engineered carboxyesterase enzymes in amidation reactions.
Catalytic acceptorless dehydrogenations: Ru-Macho catalyzed construction of amides and imines
Oldenhuis, Nathan J.,Dong, Vy M.,Guan, Zhibin
supporting information, p. 4213 - 4218 (2014/06/09)
A commercially available ruthenium(II) PNP type pincer catalyst (Ru-Macho) promotes formation of amides and imines from alcohols and amines via an acceptorless dehydrogenation pathway. The formation of secondary amides, tertiary amides, and secondary ketimines occurs in yields ranging from 35% to 95%.
Synthesis, structure and anticancer activity of copper(II) complexes of N-benzyl-2-(diethylamino)acetamide and 2-(diethylamino)-N-phenylethylacetamide
Singh, Amit P.,Kaushik, Nagendra K.,Verma, Akhilesh K.,Gupta, Rajeev
experimental part, p. 474 - 483 (2011/06/20)
The ligands N-benzyl-2-(diethylamino)acetamide, (HL1) and 2-(diethylamino)-N-phenylethylacetamide (HL2), have been used to synthesize copper(II) complexes, [Cu(HL1)2](ClO 4)2 (1) and [Cu(HL2)2](ClO 4)2 (2), respectively. Both complexes are well characterized by various spectral and physical methods. The crystal structure of complex (1) reveals that two bidentate ligands coordinate the Cu(II) ion via Oamide and Namine atoms in the basal plane whereas one of the ClO4- ions occupies the apical position maintaining a square-pyramidal geometry. Screening results for anti-proliferative studies against the U87 and HeLa cancerous cells indicate promising activity. The complexes enhanced growth inhibition and cell death in a concentration and time dependent manner for both U87 and HeLa cell lines. Of the two compounds, complex (2) exhibits better activity against both HeLa and U87 cells. Further, both complexes are specifically potent against U87 after 72 h of treatment. Micronucleus and apoptosis frequencies are 3 - 4 times higher in treated cells when compared with untreated control. Despite potent in vitro activity, both complexes exhibit diminished cytotoxicity against the normal human HEK cells at all effective concentrations.
Quantitative structure-activity relationships for N-[(N',N'-disubstituted-amino)acetyl]arylamines for local anesthetic activity and acute toxicity
Heymans,Le Therizien,Godfroid,Bessin
, p. 184 - 193 (2007/10/02)
The synthesis and physicochemical properties of a series of N-[(N',N'-disubstituted-amino)acetyl]arylamines are described. A QSAR method is applied to local anesthetic activity and acute toxicity by means of a 'nonclassic' substituent variation involving a modification on both aryl and amino moieties. The choice of the different parameters (partition coefficient, pK(a), connectivity index, molar refraction, and molar volume) is discussed and their different methods of determination are described. Molar refraction is the parameter which explains best the variance of the local anesthetic activity, and the quadratic regression with MR leads to a 'a posteriori' synthesis of one compound with optimized activity. However, the partition coefficient is the most explicative parameter for intravenous toxicity.
