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

J. Polanski; H. Niedbala; R. Musiol; B. Podeszwa; D. Tabak; A. Palka; A. Mencel; J. Finster; J.- F. Mouscadet; M. L. Bret

doi:10.2174/157018006776286934

ISSN: 1570-1808
E-ISSN: 1875-628X

5-Hydroxy-6-Quinaldic Acid as a Novel Molecular Scaffold for HIV-1 Integrase Inhibitors
Authors: J. Polanski¹, H. Niedbala², R. Musiol³, B. Podeszwa⁴, D. Tabak⁵, A. Palka⁶, A. Mencel⁷, J. Finster⁸, J.- F. Mouscadet⁹ and M. L. Bret¹⁰
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¹ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ² Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ³ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁴ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁵ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁶ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁷ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁸ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ⁹ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland. ¹⁰ Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice, Poland.
Source: Letters in Drug Design & Discovery, Volume 3, Issue 3, Apr 2006, p. 175 - 178
DOI: https://doi.org/10.2174/157018006776286934
- Available online: 01 Apr 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.

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2006-04-01

2025-10-15

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Article Type: Research Article

Keyword(s): HIV integrase inhibitors; Molecular scaffold; styrylquinolines

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

Abstract

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