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

Tamiki Nishimura; Jun etsu Igarashi; Makoto Sunagawa

doi:10.1016/S0960-894X(01)00167-6

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

Tamiki Nishimura, Jun etsu Igarashi, Makoto Sunagawa

Research output: Contribution to journal › Article › peer-review

12 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1141-1144
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	9
DOIs	https://doi.org/10.1016/S0960-894X(01)00167-6
Publication status	Published - May 7 2001
Externally published	Yes

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)00167-6

Cite this

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abstract = "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.",

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AB - 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.

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

Abstract

All Science Journal Classification (ASJC) codes

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