2. Academic Validation
  3. Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061

Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061

  • J Med Chem. 2004 Mar 25;47(7):1605-8. doi: 10.1021/jm0342414.
Montse Llinàs-Brunet 1,  Murray D Bailey,  Gordon Bolger,  Christian Brochu,  Anne-Marie Faucher,  Jean Marie Ferland,  Michel Garneau,  Elise Ghiro,  Vida Gorys,  Chantal Grand-Maître,  Ted Halmos,  Nicole Lapeyre-Paquette,  Francine Liard,  Martin Poirier,  Manon Rhéaume,  Youla S Tsantrizos,  Daniel Lamarre
Affiliations

Affiliation

  • 1 Department of Chemistry, Boehringer Ingelheim (Canada) Ltd., 2100 Cunard Street, Laval, Québec H7S 2G5, Canada. mllinas@lav.boehringer-ingelheim.com
PMID: 15027850 DOI: 10.1021/jm0342414
Abstract

From the discovery of competitive hexapeptide inhibitors, potent and selective HCV NS3 protease macrocyclic inhibitors have been identified. Structure-activity relationship studies were performed focusing on optimizing the N-terminal carbamate and the aromatic substituent on the (4R)-hydroxyproline moiety. Inhibitors meeting the potency criteria in the cell-based assay and with improved oral bioavailability in rats were identified. BILN 2061 was selected as the best compound, the first NS3 protease inhibitor reported with Antiviral activity in man.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z