Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT(1A)/D-2 affinity as potential atypical antipsychotics
(1998) Journal of Medicinal Chemistry — Vol. 41, n° 12, p. 2010-2018 (1998)
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- Abstract
- Since it was known that 5HT properties (5HT(1A) agonism or 5HT(2A) antagonism) combined with D-2 antagonism may lead to atypical antipsychotic drugs, a series of 19 benzothiazolin-2-one and benzoxazin-3-one derivatives possessing the arylpiperazine moiety Was prepared, and their binding profiles were investigated. All tested compounds displayed very high affinities for the 5HT(1A) and Da receptors. Therefore, further pharmacological studies were carried out on selected compounds (24, 27, 30, 46, and 47). This evaluation in rats clearly revealed potent antipsychotic properties along with a decrease of extrapyramidal side effects. These derivatives are currently under preclinical development.
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Citations
Taverne, T., Diouf, O., Depreux, P., Poupaert, J., Lesieur, D., Guardiola-Lemaitre, B., Renard, P., Rettori, M., Caignard, DH., & Pfeiffer, B. (1998). Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT(1A)/D-2 affinity as potential atypical antipsychotics. Journal of Medicinal Chemistry, 41(12), 2010-2018. https://doi.org/10.1021/jm970298c (Original work published 1998)