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
Affiliation:Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40-006 Katowice,Poland.
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.
