Fragment Based Approach for the Investigation of HIV-1 Integrase Inhibition

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

Abstract

HIV-1 integrase (IN) inhibition of a novel series of quinoline derivatives was investigated. The compounds were designed on the basis of quinoline molecular scaffolds that attempt to mimic the basic naphtyridine motif of the L-870810 HIV-1 IN inhibitor. It appeared that the IN inhibition of the novel compounds was limited by the electroacceptor substitution within quinoline. Although the compounds studied here indicate structural similarity to L-870810, they are much less efficient than this compound. This can be explained by differences in conformations and apparent magnesium complexing ability in the naphtyridine and quinoline based amides.

Keywords: Quinoline derivatives, HIV-1 integrase inhibition, Structure-activity relationships

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Letters in Drug Design & Discovery

Title: Fragment Based Approach for the Investigation of HIV-1 Integrase Inhibition

Volume: 4 Issue: 2

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

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Keywords: Quinoline derivatives, HIV-1 integrase inhibition, Structure-activity relationships

Abstract: HIV-1 integrase (IN) inhibition of a novel series of quinoline derivatives was investigated. The compounds were designed on the basis of quinoline molecular scaffolds that attempt to mimic the basic naphtyridine motif of the L-870810 HIV-1 IN inhibitor. It appeared that the IN inhibition of the novel compounds was limited by the electroacceptor substitution within quinoline. Although the compounds studied here indicate structural similarity to L-870810, they are much less efficient than this compound. This can be explained by differences in conformations and apparent magnesium complexing ability in the naphtyridine and quinoline based amides.

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Polanski J., Niedbala H., Musiol R., Podeszwa B., Tabak D., Palka A., Mencel A., Mouscadet J.-F. and Le Bret M., Fragment Based Approach for the Investigation of HIV-1 Integrase Inhibition, Letters in Drug Design & Discovery 2007; 4 (2) . https://dx.doi.org/10.2174/157018007779422532