N-{2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl}acetamide: an orally bioavailable melatonin receptor agonist

• Published in: Bioorganic & medicinal chemistry letters Vol. 14; no. 20; pp. 5157 - 5160
• Main Authors: Sun, Li-Qiang, Takaki, Katherine, Chen, Jie, Iben, Lawrence, Knipe, Jay O., Pajor, Lori, Mahle, Cathy D., Ryan, Elaine, Xu, Cen
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 18.10.2004; Elsevier
• Subjects: Agonist; Benzofuran; Biological and medical sciences; Medical sciences; Melatonin; Melatonin receptors; Miscellaneous; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems; Pharmacology. Drug treatments; Melatonin receptors; Melatonin; Agonist; Benzofuran; Oral administration; Benzofuran derivatives; Bioavailability; MT2 melatonin receptor; MT1 melatonin receptor; Chemical synthesis; Biological activity; Melatonin receptor
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.07.055

N-{2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl}acetamide 3a was synthesized as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with significantly low vasoconstrictive activity. N-{2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl}acetamide 3a was synthesized as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with significantly low vasoconstrictive activity.