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Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.
A set of 4-quinolone-3-carboxylic acids bearing different substituents on the condensed benzene ring was designed and synthesized as potential HIV-1 integrase inhibitors structurally related toExpand
Comparison of the effect of the GABAΒ receptor agonist, baclofen, and the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in 3 different lines of
The results of this study suggest that the strength of the reinforcing and motivational properties of alcohol differ among P, sP, and AA rats, and the GABA(B) receptor is part of the neural substrate mediating the reinforcement and motivational Properties of alcohol. Expand
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
The general loss of potency displayed by the compounds toward clinically relevant mutant strains was deeply studied through a molecular modeling approach, leading to the evidence that the dynamic of the entrance in the non-nucleoside binding pocket could represent the basis of the inhibitory activity of the molecules. Expand
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
Biological screening led to the identification of compounds with nanomolar activity toward both the highly purified recombinant human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) enzyme (wild-type and mutants) and wild-type (wt) and mutant HIV-1 strains. Expand
The 4-quinolone-3-carboxylic acid motif as a multivalent scaffold in medicinal chemistry.
This review focuses on the 4-quinolone-3-carboxylic acid motif as a privileged structure in medicinal chemistry for obtaining new compounds possessing antibacterial, antitumor, anti-HIV, and cannabinoid receptors modulating activities. Expand
Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and
The 8-methoxy derivative 4a endowed with the highest affinity and selectivity ever reported for a CB2 ligand is found to provide access to antihyperalgesic agents devoid of psychotropic effects. Expand
Characterization of COR627 and COR628, Two Novel Positive Allosteric Modulators of the GABAB Receptor
Two novel compounds, COR627 and COR628, may represent two additional tools for use in investigating the roles and functions of positive allosteric modulatory binding sites of the GABAB receptor. Expand
Synthesis and pharmacological characterization of 2-(acylamino)thiophene derivatives as metabolically stable, orally effective, positive allosteric modulators of the GABAB receptor.
Although displaying a lower potency in vitro than the reference compound GS39783, the new compounds 6, 10, and 11 exhibited a higher efficacy in vivo: combination of these compounds with a per se nonsedative dose of baclofen resulted in shorter onset and longer duration of the loss of righting reflex in mice. Expand
Design, synthesis, and pharmacological characterization of indol-3-ylacetamides, indol-3-yloxoacetamides, and indol-3-ylcarboxamides: potent and selective CB2 cannabinoid receptor inverse agonists.
The design and synthesis of three sets of indole-based ligands characterized by an acetamide, oxalylamide, or carboxamide chain, respectively, showed affinity for CB2 receptors in the nanomolar range, and moderate to good selectivity over CB1 receptors. Expand
Reduction by the Positive Allosteric Modulator of the GABAB Receptor, GS39783, of Alcohol Self-Administration in Sardinian Alcohol-Preferring Rats Exposed to the “Sipper” Procedure
The results of the present study suggest the power of the “sipper” procedure in triggering high levels of alcohol-seeking and -taking behavior in sP rats and extend to this additional procedure of alcohol self-administration the capacity of GS39783 to reduce the motivational properties of alcohol and alcohol consumption in s P rats. Expand