Bioorganic & Medicinal Chemistry Letters 2001-09-17

Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).

J Einsiedel, H Hübner, P Gmeiner

文献索引：Bioorg. Med. Chem. Lett. 11(18) , 2533-6, (2001)

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摘要

Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K(i)high=0.95nM). Mitogenesis experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from alpha-amino acids.