Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents

Peter I. Dosa; Sonja Strah-Pleynet; Honnappa Jayakumar; Martin Casper; Marc Decaire; Yifeng Xiong; Juerg Lehmann; Karoline Choi; Katie Elwell; Amy Wong; Robert R. Webb; John W. Adams; Juan Ramirez; Jeremy G. Richman; William Thomsen; Graeme Semple; Bradley R. Teegarden

doi:10.1016/j.bmcl.2009.07.073

Solubilized phenyl-pyrazole ureas as potent, selective 5-HT_2A inverse-agonists and their application as antiplatelet agents

Peter I. Dosa
, Sonja Strah-Pleynet
, Honnappa Jayakumar
, Martin Casper
, Marc Decaire
, Yifeng Xiong
, Juerg Lehmann
, Karoline Choi
, Katie Elwell
, Amy Wong
, Robert R. Webb
, John W. Adams
, Juan Ramirez
, Jeremy G. Richman
, William Thomsen
, Graeme Semple
, Bradley R. Teegarden

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Potent 5-HT_2A inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation.

Original language	English (US)
Pages (from-to)	5486-5489
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2009.07.073
State	Published - Sep 15 2009
Externally published	Yes

Keywords

5-HT
Antiplatelet
Antithrombosis

Publisher link

10.1016/j.bmcl.2009.07.073

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Dosa, P. I., Strah-Pleynet, S., Jayakumar, H., Casper, M., Decaire, M., Xiong, Y., Lehmann, J., Choi, K., Elwell, K., Wong, A., Webb, R. R., Adams, J. W., Ramirez, J., Richman, J. G., Thomsen, W., Semple, G., & Teegarden, B. R. (2009). Solubilized phenyl-pyrazole ureas as potent, selective 5-HT_2A inverse-agonists and their application as antiplatelet agents. Bioorganic and Medicinal Chemistry Letters, 19(18), 5486-5489. https://doi.org/10.1016/j.bmcl.2009.07.073

Dosa, PI, Strah-Pleynet, S, Jayakumar, H, Casper, M, Decaire, M, Xiong, Y, Lehmann, J, Choi, K, Elwell, K, Wong, A, Webb, RR, Adams, JW, Ramirez, J, Richman, JG, Thomsen, W, Semple, G & Teegarden, BR 2009, 'Solubilized phenyl-pyrazole ureas as potent, selective 5-HT_2A inverse-agonists and their application as antiplatelet agents', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 18, pp. 5486-5489. https://doi.org/10.1016/j.bmcl.2009.07.073

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abstract = "Potent 5-HT2A inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation.",

keywords = "5-HT, Antiplatelet, Antithrombosis",

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AU - Casper, Martin

AU - Decaire, Marc

AU - Xiong, Yifeng

AU - Lehmann, Juerg

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AU - Elwell, Katie

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AU - Ramirez, Juan

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