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In the study, a series of twelve ring-substituted 4-hydroxy-1H-quinolin-2-one derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity and tested for their photosynthesis-inhibiting activity using spinach (Spinacia oleracea L.) chloroplasts. All the synthesized compounds were also evaluated for antifungal activity using in vitro screening with eight fungal strains. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).

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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.

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.