53159-75-4Relevant academic research and scientific papers
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin
Teno, Naoki,Gohda, Keigo,Wanaka, Keiko,Tsuda, Yuko,Sueda, Takuya,Yamashita, Yukiko,Otsubo, Tadamune
, p. 2339 - 2352 (2014/04/17)
In the development of plasmin inhibitors, a novel chemotype, pyrrolopyrimidine scaffold possessing two motifs, a hydantoin-containing P4 moiety and a warhead-containing P1 moiety, is uncovered. A unique feature of the new line of the plasmin inhibitors is
Mild, convenient and versatile Cu-mediated synthesis of N-aryl-2-imidazolidinones
Stabile, Paolo,Lamonica, Alessandro,Ribecai, Arianna,Castoldi, Damiano,Guercio, Giuseppe,Curcuruto, Ornella
supporting information; experimental part, p. 3232 - 3235 (2010/08/07)
A mild, general, convenient and practical methodology for the selective copper-mediated mono N-arylation of unprotected 2-imidazolidinone was developed. Strong electron-donating groups and free hydroxy and amino groups on the aryl iodide substrates were well tolerated. The use of n-butanol as the solvent for the copper-catalysed mono-arylation of 2-imidazolidinone is unprecedented.
2,4-SUBSTITUTED PYRIMIDINES AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 72-73, (2010/10/20)
Substituted heteroaryl nitrile derivatives of Formula (I) processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α2-adrenoceptor antagonist activity
Mayer,Brunel,Chaplain,Piedecoq,Calmel,Schambel,Chopin,Wurch,Pauwels,Marien,Vidaluc,Imbert
, p. 3653 - 3664 (2007/10/03)
The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α2-adrenoceptor antagonists with good selectivity versus α1-adrenergic and D2-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α2-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.
