Details

Autor(en) / Beteiligte

• St. Laurent, Denis R.
• Serrano-Wu, Michael H.
• Belema, Makonen
• Ding, Min
• Fang, Hua
• Gao, Min
• Goodrich, Jason T.
• Krause, Rudolph G.
• Lemm, Julie A.
• Liu, Mengping
• Lopez, Omar D.
• Nguyen, Van N.
• Nower, Peter T.
• O’Boyle, Donald R.
• Pearce, Bradley C.
• Romine, Jeffrey L.
• Valera, Lourdes
• Sun, Jin-Hua
• Wang, Ying-Kai
• Yang, Fukang
• Yang, Xuejie
• Meanwell, Nicholas A.
• Snyder, Lawrence B.

Titel

HCV NS5A Replication Complex Inhibitors. Part 4. Optimization for Genotype 1a Replicon Inhibitory Activity

Ist Teil von

• Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1976-1994

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2014

Quelle

MEDLINE

Beschreibungen/Notizen

• A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging from an examination of the prolinamide cap region revealed 11 to be a selective HCV NS5A inhibitor exhibiting submicromolar potency against both G-1a and G-1b replicons. Additional structural refinements resulted in the identification of 30 as a potent, dual G-1a/1b HCV NS5A inhibitor.