873673-51-9Relevant academic research and scientific papers
Syntheses of 5-amino-2-phenyl-4(3H)-pyrimidinone derivertives starting with glycine
Takahashi, Daisuke,Honda, Yutaka,Izawa, Kunisuke
, p. 1089 - 1103 (2012/08/07)
N-Cbz derivative of 5-amino-2-phenyl-4(3H)-pyrimidinone was prepared from sodium salt of methyl hydroxymethylene glycinate and benzamidine hydrochloride in good yield. However, the reaction with N-substituted benzamidine did not proceed to give the desired pyrimidinone. In contrast, the reaction of 4-ethoxymethylene-2-phenyl-5(4H)-oxazolone readily prepared from hippuric acid and N-substituted benzamidine proceeded nicely to give 5-(benzoylamino)-6-oxo-2- phenyl-1(6H)-pyrimidineacetic acid in high yield.
Design and synthesis of new orally active inhibitors of human neutrophil elastase
Ohmoto, Kazuyuki,Okuma, Motohiro,Yamamoto, Tetsuya,Kijima, Hideomi,Sekioka, Tomohiko,Kitagawa, Kanji,Yamamoto, Shigeki,Tanaka, Kenji,Kawabata, Kazuhito,Sakata, Atsushi,Imawaka, Haruo,Nakai, Hisao,Toda, Masaaki
, p. 1307 - 1323 (2007/10/03)
To identify new orally active inhibitors, further modification of 1 (ONO-6818) was performed. Peptidic derivatives 4b, 4c and 4n showed more potent inhibitory activity than nonpeptidic derivatives 3a-c. As a result, a series of peptidic inhibitors, 4a-s a
Pyridone-based peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE)
Semple, Graeme,Ashworth, Doreen M.,Baker, Graham R.,Batt, Andrzej R.,Baxter, Andrew J.,Benzies, David W.M.,Elliot, Lucy H.,Evans, D. Michael,Franklin, Richard J.,Hudson, Peter,Jenkins, Paul D.,Pitt, Gary R.,Rooker, David P.,Sheppard, Andrew,Szelke, Michael,Yamamoto, Satoshi,Isomura, Yasuo
, p. 1337 - 1342 (2007/10/03)
New potent, reversible inhibitors of recombinant human Interleukin-1 β-converting enzyme (ICE, caspase-1) with significantly reduced peptide character are described. The compounds were designed by incorporation of pyridone and pyrimidone heterocyclic replacements for the P2-P3 amino acids of the native substrate and were optimised by manipulation of peripheral alkyl and aryl substituents.
