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
Letters in Drug Design & Discovery
Title: 5-Hydroxy-6-Quinaldic Acid as a Novel Molecular Scaffold for HIV-1 Integrase Inhibitors
Volume: 3 Issue: 3
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
Affiliation:
Keywords: Molecular scaffold, HIV integrase inhibitors, styrylquinolines
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.
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Cite this article as:
Polanski J., Niedbala H., Musiol R., Podeszwa B., Tabak D., Palka A., Mencel A., Finster J., Mouscadet F. J.- and Bret L. M., 5-Hydroxy-6-Quinaldic Acid as a Novel Molecular Scaffold for HIV-1 Integrase Inhibitors, Letters in Drug Design & Discovery 2006; 3 (3) . https://dx.doi.org/10.2174/157018006776286934
DOI https://dx.doi.org/10.2174/157018006776286934 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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