161175-83-3Relevant academic research and scientific papers
Fragment-Based Identification of Influenza Endonuclease Inhibitors
Credille, Cy V.,Chen, Yao,Cohen, Seth M.
, p. 6444 - 6454 (2016)
The influenza virus is responsible for millions of cases of severe illness annually. Yearly variance in the effectiveness of vaccination, coupled with emerging drug resistance, necessitates the development of new drugs to treat influenza infections. One a
Synthesis and evaluation of heterocyclic catechol mimics as inhibitors of catechol-o-methyltransferase (COMT)
Harrison, Scott T.,Poslusney, Michael S.,Mulhearn, James J.,Zhao, Zhijian,Kett, Nathan R.,Schubert, Jeffrey W.,Melamed, Jeffrey Y.,Allison, Timothy J.,Patel, Sangita B.,Sanders, John M.,Sharma, Sujata,Smith, Robert F.,Hall, Dawn L.,Robinson, Ronald G.,Sachs, Nancy A.,Hutson, Pete H.,Wolkenberg, Scott E.,Barrow, James C.
supporting information, p. 318 - 323 (2015/03/30)
3-Hydroxy-4-pyridinones and 5-hydroxy-4-pyrimidinones were identified as inhibitors of catechol-O-methyltransferase (COMT) in a high-throughput screen. These heterocyclic catechol mimics exhibit potent inhibition of the enzyme and an improved toxicity profile versus the marketed nitrocatechol inhibitors tolcapone and entacapone. Optimization of the series was aided by X-ray cocrystal structures of the novel inhibitors in complex with COMT and cofactors SAM and Mg2+. The crystal structures suggest a mechanism of inhibition for these heterocyclic inhibitors distinct from previously disclosed COMT inhibitors.
Synthesis of N-Substituted 3-Hydroxy-2-methyl-4-pyridones and -pyridonimines
Faerber, M.,Osiander, H.,Severin, T.
, p. 947 - 956 (2007/10/02)
Carbohydrates with 1,4-glycoside bonds like maltose, lactose, dextrin or strach react with primary amines as well as amino acids or proteins to give i.e. 3-hydroxy-2-methyl-4-pyridones 5 and 3-hydroxy-2-methyl-4-pyridonimines 7.A generally applicable synt
