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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Author(s): J. Polanski, H. Niedbala, R. Musiol, B. Podeszwa, D. Tabak, A. Palka, A. Mencel, J. Finster, J.- F. Mouscadet and M. L. Bret

Volume 3, Issue 3, 2006

Page: [175 - 178] Pages: 4

DOI: 10.2174/157018006776286934

Price: $65

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.

Keywords: Molecular scaffold, HIV integrase inhibitors, styrylquinolines


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