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

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

Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 2 , 2007

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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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Article Details

VOLUME: 4
ISSUE: 2
Year: 2007
Page: [99 - 105]
Pages: 7
DOI: 10.2174/157018007779422532
Price: $58