Conformational analysis of tandospirone in aqueous solution: lead evolution of potent dopamine D4 receptor ligands

T Nishimura, J Igarashi, M Sunagawa

文献索引：Nishimura, Tamiki; Igarashi, Jun-etsu; Sunagawa, Makoto Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 9 p. 1141 - 1144

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被引用次数: 13

摘要

The significant contribution of folded conformation (2) of the anxiolytic tandospirone (1) in aqueous solution was verified by dynamic 1H NMR. A structurally rigid mimic of 2 was designed and synthesized to evaluate the implication of 2 towards neuroleptic receptor binding. The designed structures provided a new rigid scaffold for dopamine D4 ligands.