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5-Hydroxy-6-Quinaldic Acid as a Novel Molecular Scaffold for HIV-1 Integrase Inhibitors

Authors :
Polanski, J.
Niedbala, H.
Musiol, R.
Podeszwa, B.
Tabak, D.
Palka, A.
Mencel, A.
Finster, J.
Mouscadet, J.- F.
Bret, M. L.
Source :
Letters in Drug Design & Discovery; April 2006, Vol. 3 Issue: 3 p175-178, 4p
Publication Year :
2006

Abstract

8-Hydroxy-7-quinaldic acid can be considered as a basic scaffold for all reported styrylquinoline HIV-1 integrase inhibitors. However, when tested in vitro, this compound appeared to be inactive against the enzyme. We have designed and synthesized an improved molecular fragment, i.e. 5-hydroxy-8-nitro-6-quinaldic acid, which appeared to inhibit HIV-1 integrase in vitro.

Details

Language :
English
ISSN :
15701808
Volume :
3
Issue :
3
Database :
Supplemental Index
Journal :
Letters in Drug Design & Discovery
Publication Type :
Periodical
Accession number :
ejs14720019