Löber S, Gmeiner P, Hübner H (2002)
Publication Type: Journal article
Publication year: 2002
Publisher: Elsevier
Book Volume: 12
Pages Range: 2377-2380
DOI: 10.1016/S0960-894X(02)00390-6
Computational studies based on the similarity of molecular electrostatic potential maps initiated the synthesis of the tricyclic target compounds 1 (FAUC 725) and 2. Receptor binding studies at the dopamine receptor subtypes D1, D2long, D2short, D3 and D4 showed that the azaindole 1 revealed D3 affinity (Ki=0.54 nM) comparable to the lead pramipexole and enhanced selectivity over D2 and D4. Mitogenesis experiments indicated substantial intrinsic activity for the D3 selective dipropylamine 1. Based on the structure of (S)-3-PPP, bioisosteric replacement and conformational restriction leading to the test compound 2 was not fruitful. © 2002 Elsevier Science Ltd. All rights reserved.
APA:
Löber, S., Gmeiner, P., & Hübner, H. (2002). Fused Azaindole Derivatives: Molecular Design, Synthesis and in vitro Pharmacology Leading to the Preferential Dopamine D3 Receptor Agonist FAUC 725. Bioorganic & Medicinal Chemistry Letters, 12, 2377-2380. https://doi.org/10.1016/S0960-894X(02)00390-6
MLA:
Löber, Stefan, Peter Gmeiner, and Harald Hübner. "Fused Azaindole Derivatives: Molecular Design, Synthesis and in vitro Pharmacology Leading to the Preferential Dopamine D3 Receptor Agonist FAUC 725." Bioorganic & Medicinal Chemistry Letters 12 (2002): 2377-2380.
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