Discovery of ITX 4520: A highly potent orally bioavailable hepatitis C virus entry inhibitor

DOI: 10.1016/j.bmcl.2012.06.038

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 4955 - 4961 (2012)

Update date:2022-08-03

Topics:

Authors:

Mittapalli, Gopi Kumar

Zhao, Fang

Jackson, Andrew

Gao, Hongfeng

Lee, Haekyung

Chow, Stephine

Kaur, Maninder Pal

Nguyen, Natalie

Zamboni, Robert

McKelvy, Jeffrey

Wong-Staal, Flossie

MacDonald, James E.

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/j.bmcl.2012.06.038

The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral exposure, half-life and oral bioavailability. The compound is also well-tolerated in the preliminary in vivo toxicity studies and has been selected as a pre-clinical candidate for our HCV clinical pipeline.

Full text of DOI:10.1016/j.bmcl.2012.06.038

Products guided by the article

Product name:C₁₅H₁₄IN₃O₂

Cas No:1392116-46-9

R&D Labs maybe for 1392116-46-9

Suzhou Ryan Pharmachem Technology Co.,Ltd

Contact:+86-0512-68780025

Address:B-301,No.2 Taishan Road,Suzhou New District,Jiangsu,P.R. China
Nanjing Norris Pharm Technology Co., Ltd.

Contact:+86-13901585132

Address:2 Qiande Road, Jiangning sciencepark Hi-Tech Zone, Nanjing, P.R.China
Jiangxi Hessence Chemicals Co., Ltd.

Contact:+86 796 3511924

Address:Chengxi Industrial Park, Jishui County, Jiangxi Province 331600 China.
shanghai Tauto Biotech Co., Ltd

website:http://www.tautobiotech.com/en/index.htm

Contact:+86-21-51320588 ext. 8025

Address:No. 326, Aidisheng Rd , Zhangjiang Hi-tech Park, Shanghai , P.R.CHINA
Taizhou Shengxing Chempharm Co.,Ltd

Contact:+86-576-88516600

Address:Yantou Chemical Zone Jiaojiang Taizhou Zhejiang China

Relevant to this article

Carnosine analogues containing NO-donor substructures: Synthesis, physico-chemical characterization and preliminary pharmacological profile

Doi:10.1016/j.ejmech.2012.04.032
(2012)
Total Synthesis of (+)-Bicyclohumulenone

Doi:10.1246/cl.1992.167
(1992)
Synthesis of new bis (aminoethanethiol) (BAT) derivatives: Possible ligands for ^99mTc brain imaging agents

Doi:10.1021/jm00147a028
(1985)
Discovery and Characterization of R/S-N-3-Cyanophenyl-N′-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea, a New Histone Deacetylase Class III Inhibitor Exerting Antiproliferative Activity against Cancer Cell Lines

Doi:10.1021/acs.jmedchem.7b00533
(2017)
Asymmetric hydrogenation of 2,4-disubstituted 1,5-benzodiazepines using cationic ruthenium diamine catalysts: An unusual achiral counteranion induced reversal of enantioselectivity

Doi:10.1002/anie.201200309
(2012)
Radical pathway in catecholase activity with zinc-based model complexes of compartmental ligands

Doi:10.1021/ic300400v
(2012)

Article Doi