The identification of highly efficacious functionalised tetrahydrocyclopenta[<i>c</i>]pyrroles as inhibitors of HBV viral replication through modulation of HBV capsid assembly-Reference-Cited by-同舟云学术

The identification of highly efficacious functionalised tetrahydrocyclopenta[c]pyrroles as inhibitors of HBV viral replication through modulation of HBV capsid assembly

Published:2022 Issue:3 Volume:13 Page:343-349
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Cole Andrew G.¹^ORCID,Kultgen Steven G.¹,Mani Nagraj¹,Ardzinski Andrzej¹,Fan Kristi Yi¹,Thi Emily P.¹^ORCID,Dorsey Bruce D.¹,Stever Kim¹,Chiu Tim¹,Tang Sunny¹^ORCID,Daly Owen¹,Phelps Janet R.¹,Harasym Troy¹,Olland Andrea²,Suto Robert K.²^ORCID,Sofia Michael J.¹

Affiliation:

1. Arbutus Biopharma, Inc., 701 Veterans Circle, Warminster, PA 18974, USA

2. Xtal BioStructures Inc., 12 Michigan Drive, Natick, MA 01760, USA

Abstract

Pharmacokinetic optimisation of the clinical candidate HBV capsid inhibitor AB-506 resulted in dramatic improvements in oral exposure and half-life providing compound 17 which demonstrated low dose QD efficacy in a mouse model of HBV replication.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D1MD00318F

Reference33 articles.

1. Current treatments for chronic hepatitis B virus infections

2. New Therapeutics for Hepatitis B: The Road to Cure

3. Nucleoside/nucleotide analog inhibitors of hepatitis B virus polymerase: mechanism of action and resistance

4. Research priorities for the discovery of a cure for chronic hepatitis B: Report of a workshop

5. Modulators of HBV capsid assembly as an approach to treating hepatitis B virus infection

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