DSpace at KIST: Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands

Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands

Authors: Cha, MY; Choi, BC; Kang, KH; Pae, AN; Choi, KI; Cho, YS; Koh, HY; Lee, HY; Jung, D; Kong, JY

Citation: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.12, no.10, pp.1327 - 1330

Abstract: A piperazinylbutylisoxazole libary was designed, synthesized and screened for the binding affinities to dopamine D-2, D-3, and D-4 receptors. Several ligands were identified to possess high binding affinity and selectivity for the D-3 and D-4 receptors over the D-2 receptor. Compounds 6s and 6t showed K-i values of 2.6 nM and 3.9 nM for the D-3 receptor with 46- and 50-fold selectivity over the D-3 receptor, respectively. (C) 2002 Elsevier Science Ltd. All rights reserved.

Keywords: MOLECULAR-CLONING; HIGH-AFFINITY; D-3 RECEPTOR; ANTAGONIST; GENE; HALOPERIDOL; EFFICACY; AGONIST; CYCLASE; POTENT; MOLECULAR-CLONING; HIGH-AFFINITY; D-3 RECEPTOR; ANTAGONIST; GENE; HALOPERIDOL; EFFICACY; AGONIST; CYCLASE; POTENT; piperazinyalkylisoxazole

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