Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists

T Yasunaga, T Kimura, R Naito, T Kontani…

Index: Yasunaga, Tomoyuki; Kimura, Takenori; Naito, Ryo; Kontani, Toru; Wanibuchi, Fumikazu; Yamashita, Hiroshi; Nomura, Tamako; Tsukamoto, Shin-Ichi; Yamaguchi, Tokio; Mase, Toshiyasu Journal of Medicinal Chemistry, 1998 , vol. 41, # 15 p. 2765 - 2778

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Citation Number: 12

Abstract

A series of novel 6-fluorochroman derivatives was prepared and evaluated as antagonists for the 5-HT1A receptor. N-2-[[(6-Fluorochroman-8-yl) oxy] ethyl]-4-(4-methoxyphenyl) butylamine (3; J. Med. Chem. 1997, 40, 1252-1257) was chosen as a lead, and structural modifications were done on the aliphatic portion of the chroman ring, the tether linking the middle amine and the terminal aromatic ring, the aromatic ring, and lastly the amine. ...

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