166818-87-7Relevant articles and documents
Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor
Paparin, Jean-Laurent,Amador, Agnès,Badaroux, Eric,Bot, Stéphanie,Caillet, Catherine,Convard, Thierry,Da Costa, Daniel,Dukhan, David,Griffe, Ludovic,Griffon, Jean-Fran?ois,LaColla, Massimiliano,Leroy, Frédéric,Liuzzi, Michel,Giulia Loi, Anna,McCarville, Joe,Mascia, Valeria,Milhau, Julien,Onidi, Loredana,Pierra, Claire,Rahali, Rachid,Rosinosky, Elodie,Sais, Efisio,Seifer, Maria,Surleraux, Dominique,Standring, David,Dousson, Cyril B.
, p. 2634 - 2640 (2017/05/10)
Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells, and as a consequence is an attractive target for selective inhibition. This paper describes the discovery of a novel family of HCV NS5B non-nucleoside inhibitors inspired by the bioisosterism between sulfonamide and phosphonamide. Systematic structural optimization in this new series led to the identification of IDX375, a potent non-nucleoside inhibitor that is selective for genotypes 1a and 1b. The structure and binding domain of IDX375 were confirmed by X-ray co-crystalisation study.
Synthesis of 5- and 6-membered heterocycles by a strategy combining SNAr and SRN1 reactions
Beugelmans, Rene,Chbani, Mohamed
, p. 306 - 313 (2007/10/02)
The SRN1 mechanism is compatible with many substituents on the benzenic substrate and allows SRN1 reactions to be combined with SNAr reactions in a strategy which brings together their corresponding synthetic advantages.Thus, compounds containing benzene fused to 5- or 6-membered heterocycles containing N (indoles), N and P (benzazaphospholes) and N and S (benzothiazines) are readily obtained. nucleophilic aromatic substitution / SRN1 / SNAr / benzene-fused heterocycles
