Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Bioorg Med Chem Lett
; 18(19): 5307-10, 2008 Oct 01.
Article
in En
| MEDLINE
| ID: mdl-18774711
ABSTRACT
HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell. Integrase inhibitor N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide selectively inhibits the strand transfer process of integration. 4-Substituted pyrrolidinones possessing various groups on the pyrrolidinone nitrogen were introduced at the 5-position of the naphthyridine scaffold. These analogs exhibit excellent activity against viral replication in a cell-based assay. The preparation of these compounds was enabled by a three-step, two-pot reaction sequence from a common butenolide intermediate.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
HIV-1
/
HIV Integrase Inhibitors
/
HIV Integrase
/
Anti-HIV Agents
/
Naphthyridines
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country:
United States