Oxidant-Free C(sp2)-H Functionalization/C-O Bond Formation: A Kolbe Oxidative Cyclization Process
An anodic oxidation/cyclization of 2-arylbenzoic acids for the synthesis of dibenzopyranones has been developed. The reaction proceeds at room temperature with no oxidant or electrolyte required and exhibits a high atom economy with H2 being th
Chronobiotic activity of N-[2-(2,7-dimethoxyfluoren-9-yl)ethyl]- propanamide. Synthesis and melatonergic pharmacology of fluoren-9-ylethyl amides
Compound 2b demonstrated full agonism at both human MT1 and MT2 receptors and demonstrated chronobiotic activity in both acute and chronic rat models, producing an acute phase advance of 32 min at 1 mg/kg and chronically entraining free-running rats with a mean effective dose of 0.23 mg/kg. This compound was significantly less efficacious than melatonin in constricting human coronary artery. A series of fluoren-9-yl ethyl amides (2) were synthesized and evaluated for human melatonin MT1 and MT 2 receptor binding. N-[2-(2,7-dimethoxyfluoren-9-yl)ethyl]propanamide (2b) was selected and evaluated in functional assays measuring intrinsic activity at the human MT1 and MT2 receptors and demonstrated full agonism at both receptors. The chronobiotic properties of 2b were demonstrated in both acute and chronic rat models where 2b produced an acute phase advance of 32 min at 1 mg/kg and chronically entrained free-running rats with a mean effective dose of 0.23 mg/kg. Compound 2b is significantly less efficacious than melatonin in constricting human coronary artery.
Epperson, James R.,Bruce, Marc A.,Catt, John D.,Deskus, Jeffrey A.,Hodges, Donald B.,Karageorge, George N.,Keavy, Daniel J.,Mahle, Cathy D.,Mattson, Ronald J.,Ortiz, Astrid A.,Parker, Michael F.,Takaki, Katherine S.,Watson, Brett T.,Yevich, Joseph P.
p. 4601 - 4611
(2007/10/03)
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