Alexandre, Francois-Rene; Brandt, Guillaume; Caillet, Catherine; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Musiu, Chiara; Parsy, Christophe; Rahali, Houcine; Roques, Virginie; Seifer, Maria; Standring, David; Surleraux, Dominique published the artcile< Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease>, Computed Properties of 25999-04-6, the main research area is homoserine based macrocycle preparation HCV NS34A inhibitor SAR; HCV NS3/4A protease inhibitors; Hepatitis C; Macrocycle; Synthesis and biological evaluation.
We disclose here the synthesis of a series of macrocyclic HCV protease inhibitors, where the homoserine linked together the quinoline P2′ motif and the macrocyclic moiety. These compounds exhibit potent inhibitory activity against HCV NS3/4A protease and replicon cell based assay. Their enzymic and antiviral activities are modulated by substitutions on the quinoline P2′ at position 8 by Me and halogens and by small heterocycles at position 2. The in vitro structure activity relationship (SAR) studies and in vivo pharmacokinetic (PK) evaluations of selected compounds are described herein.
Bioorganic & Medicinal Chemistry Letters published new progress about Hepatitis C. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Computed Properties of 25999-04-6.
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