Anti-HBV specific β-L-2′-deoxynucleosides

被引：23

作者：

Bryant, ML

Bridges, EG

Placidi, L

Faraj, A

Loi, AG

Pierra, C

Dukhan, D

Gosselin, G

Imbach, JL

Hernandez, B

Juodawlkis, A

Tennant, B

Korba, B

Cote, P

Cretton-Scott, E

Schinazi, RF

Sommadossi, JP

机构：

[1] Novirio Pharmaceut Inc, Cambridge, MA 02476 USA

[2] Univ Alabama, Dept Pharmacol & Toxicol, Div Clin Pharmacol, Ctr Liver, Birmingham, AL 35294 USA

[3] Novirio Pharmaceut, SARL, F-75008 Paris, France

[4] Univ Montpellier 2, CNRS, UMR 5625, Chim Bioorgan Lab, F-34095 Montpellier 5, France

[5] Cornell Univ, Coll Vet Med, Dept Clin Sci, Ithaca, NY 14853 USA

[6] Georgetown Univ, Coll Med, Div Mol Virol & Immunol, Rockville, MD 20852 USA

[7] Emory Univ, Sch Med, Dept Pediat, Biochem Pharmacol Lab, Decatur, CA USA

[8] Vet Affairs Med Ctr, Decatur, CA USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2001年 / 20卷 / 4-7期

关键词：

D O I：

10.1081/NCN-100002336

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A unique series of simple unnatural L-nucleosides that specifically inhibit hepatitis B virus (HBV) replication has been discovered. These molecules have in common a hydroxyl group in the 3'-position (3'-OH) of the beta -L-2'-deoxyribose sugar that confers antiviral activity specifically against hepadnaviruses. Replacement of the 3'-OH broadens activity to other viruses, Substitution in the base decreases antiviral potency and selectivity. Human DNA polymerases and mitochondrial function are not effected. Plasma viremia is reduced up to 8 logs in a woodchuck model of chronic HBV infection. These investigational drugs, used alone or in combination, are expected to offer new therapeutic options for patients with chronic HBV infection.

引用

页码：597 / 607

页数：11

共 38 条

[1] Anti-human immunodeficiency and anti-hepatitis B virus activities of beta-L-2',3'-dideoxy purine nucleosides [J].