Synthesis, SAR studies, and evaluation of 1, 4-benzoxazepine derivatives as selective 5-HT 1A receptor agonists with neuroprotective effect: Discovery of Piclozotan

…, R Katsuragi-Ogino, M Koyama, M Nakajima…

Index: Kamei, Katsuhide; Maeda, Noriko; Nomura, Kayoko; Shibata, Makoto; Katsuragi-Ogino, Ryoko; Koyama, Makoto; Nakajima, Mika; Inoue, Teruyoshi; Ohno, Tomochika; Tatsuoka, Toshio Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 6 p. 1978 - 1992

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Citation Number: 50

Abstract

A new series of 1, 4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1, 2, 3, 6-tetrahydropyridin-1-yl] butyl]-1, 4-benzoxazepin-5 (4H)-one (50: SUN N4057 ( ...