Details

Autor(en) / Beteiligte

• Yu, Wensheng
• Hu, Bin
• Zhong, Bin
• Hao, Jinglai
• Lei, Zhixin
• Agrawal, Sony
• Rokosz, Laura
• Liu, Rong
• Chen, Shiying
• Asante-Appiah, Ernest
• Kozlowski, Joseph A.

Titel

Discovery of novel pan-genotypic HCV NS5A inhibitors containing a novel tetracyclic core

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2019-03, Vol.29 (5), p.700-706

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2019

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• [Display omitted] A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino acid moiety improved their potency and yielded HCV NS5A inhibitors with a minimum potency shift from the GT1a strain compared to other genotypes and mutants. Compounds 53 and 54 showed the best potency profile and had reasonable half-times in rat PK studies. However, further optimization of their oral bioavailability is still needed in order to advance them for further development. [BMCL ABSTRACT] ©2000 Elsevier Science Ltd. All rights reserved.