Benzamide Bioisosteres Incorporating Dihydroheteroazole Substructures: EPC Synthesis and SAR Leading to a Selective Dopamine D4 Receptor Partial Agonist (FAUC 179)

Gmeiner P, Einsiedel J, Hübner H (2001)

Publication Type: Journal article

Publication year: 2001

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 11

Pages Range: 2533-2536

DOI: 10.1016/S0960-894X(01)00484-X

Abstract

Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (Kihigh = 0.95 nM). Mitogenesis experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from α-amino acids. © 2001 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. (2001). Benzamide Bioisosteres Incorporating Dihydroheteroazole Substructures: EPC Synthesis and SAR Leading to a Selective Dopamine D4 Receptor Partial Agonist (FAUC 179). Bioorganic & Medicinal Chemistry Letters, 11, 2533-2536. https://doi.org/10.1016/S0960-894X(01)00484-X

MLA:

Gmeiner, Peter, Jürgen Einsiedel, and Harald Hübner. "Benzamide Bioisosteres Incorporating Dihydroheteroazole Substructures: EPC Synthesis and SAR Leading to a Selective Dopamine D4 Receptor Partial Agonist (FAUC 179)." Bioorganic & Medicinal Chemistry Letters 11 (2001): 2533-2536.

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