imidazolone and Disease-Models--Animal

Aldose reductase (ALR2) inhibitors provide a viable mode to fight against diabetic complications. ALR2 exhibit plasticity in the active site vicinities and possible shifts in the nearby two supporting alpha helices. Therefore, a novel series of amino acid conjugates of chromene-3-imidazoles (13-15) were designed and synthesized based on natural isoflavonoids. The compounds were identified on the basis of spectral (

Topics: Aldehyde Reductase; Amino Acids; Animals; Benzopyrans; Blood Glucose; Catalytic Domain; Cataract; Diabetes Complications; Disease Models, Animal; Drug Design; Enzyme Activation; Enzyme Inhibitors; Imidazoles; Inhibitory Concentration 50; Molecular Docking Simulation; Rats; Stereoisomerism; Structure-Activity Relationship

This communication describes the synthesis and in vitro PDE4 inhibitory activity of a novel series of imidazol-2-one and 2-cyanoiminoimidazole derivatives. The compounds described were also tested in in vivo models to evaluate their anti-inflammatory activity after topical administration as well as their gastro-intestinal side effects. Several compounds proved to be potent PDE4 inhibitors and some 2-cyanoiminoimidazoles showed less pronounced gastro-intestinal side effects than reference compounds but maintained anti-inflammatory activity after topical administration.

Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Topical; Animals; Anti-Inflammatory Agents; Cyclic Nucleotide Phosphodiesterases, Type 4; Disease Models, Animal; Dose-Response Relationship, Drug; Ear Diseases; Enzyme Inhibitors; Humans; Imidazoles; Inflammation; Inhibitory Concentration 50; Rats; Structure-Activity Relationship