Cyclic Amidines as Benzamide Bioisosteres: EPC Synthesis and SAR Studies Leading to the Selective Dopamine D4 Receptor Agonist FAUC 312

Gmeiner P, Einsiedel J, Hübner H (2003)

Publication Type: Journal article

Publication year: 2003

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 13

Pages Range: 851-854

DOI: 10.1016/S0960-894X(03)00004-0

Abstract

Investigation of conformationally restricted benzamide bioisosteres led to the chiral phenyltetrahydropyrimidine derivative ent2a (FAUC 312) displaying strong and highly selective dopamine D4 receptor binding (Kihigh=1.5 nM). Mitogenesis experiments indicated 83% ligand efficacy when compared to the unselective agonist quinpirole. The target compounds of type 2 and 3 were synthesized in enantiopure form starting from asparagine. © 2003 Elsevier Science Ltd. All rights reserved.

Authors with CRIS profile

Peter Gmeiner Lehrstuhl für Pharmazeutische Chemie Jürgen Einsiedel Lehrstuhl für Pharmazeutische Chemie Harald Hübner Lehrstuhl für Pharmazeutische Chemie

How to cite

APA:

Gmeiner, P., Einsiedel, J., & Hübner, H. (2003). Cyclic Amidines as Benzamide Bioisosteres: EPC Synthesis and SAR Studies Leading to the Selective Dopamine D4 Receptor Agonist FAUC 312. Bioorganic & Medicinal Chemistry Letters, 13, 851-854. https://doi.org/10.1016/S0960-894X(03)00004-0

MLA:

Gmeiner, Peter, Jürgen Einsiedel, and Harald Hübner. "Cyclic Amidines as Benzamide Bioisosteres: EPC Synthesis and SAR Studies Leading to the Selective Dopamine D4 Receptor Agonist FAUC 312." Bioorganic & Medicinal Chemistry Letters 13 (2003): 851-854.

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