Bioorganic and Medicinal Chemistry Letters p. 2579 - 2584 (1997)
Update date:2022-08-05
Topics:
Diouf
Carato
Depreux
Bonte
Caignard
Guardiola-Lemaitre
Rettori
Belzung
Lesieur, Daniel
A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazin-3-one derivatives were synthesized and their binding profile at 5-HT(1A) 5-HT(2A), 5-HT(2C) as well as D2 and α1 receptors was determined. All studied compounds displayed high to moderate affinity for both 5-HT(1A) and 5-HT(2A) receptor subtypes. Among these, one compound (29) emerged since it exhibited potent antagonist activities at 5-HT(1A), 5-HT(2A), D2 and α1 central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation.
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Doi:10.1021/ja00267a033
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