956109-57-2Relevant academic research and scientific papers
Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates
Li, Pan,Dorsch, Warren,Lauffer, David J.,Bilimoria, Darius,Chauret, Nathalie,Court, John J.,Das, Sanjoy Kumar,Denis, Francois,Mani, Nagraj,Nanthakumar, Suganthini,Nicolas, Olivier,Rao, B. Govinda,Ronkin, Steven,Selliah, Subajini,Shawgo, Rebecca S.,Stearns, Ralph,Tang, Qing,Waal, Nathan D.,Green, Jeremy
, p. 251 - 255 (2017)
Lomibuvir (1) is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase with demonstrated clinical efficacy. Further development efforts within this class of inhibitor focused on improving the antiviral activity and physicochemical and pharmacokinetic properties. Recently, we reported the development of this series, leading to compound 2, a molecule with comparable potency and an improved physicochemical profile relative to 1. Further exploration of the amino amide-derived side chain led to a series of lactam derivatives, inspired by the X-ray crystal structure of related thiophene carboxylate inhibitors. This series, exemplified by 12f, provided 3-5-fold improvement in potency against HCV replication, as measured by replicon assays. The synthesis, structure-activity relationships, in vitro ADME characterization, and in vivo evaluation of this novel series are discussed.
Synthesis of optically active medium-sized α-aminolactams via ring-closing metathesis
Fuhshuku, Ken-Ichi,Asano, Yasuhisa
experimental part, p. 6651 - 6655 (2012/08/29)
The synthesis of optically active medium-sized α-aminolactams via ring-closing metathesis is described. The amidation of optically active N-Boc-allylglycine derivatives with N-protected alkenylamine, and ring-closing metathesis resulted in the formation o
P38 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 72, (2008/06/13)
Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.
