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 journalArticle

10 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 languageEnglish
Pages (from-to)1141-1144
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number9
DOIs
Publication statusPublished - May 7 2001

Fingerprint

Dopamine D4 Receptors
Anti-Anxiety Agents
Scaffolds
Conformations
Dopamine
Nuclear magnetic resonance
Ligands
neurotensin mimic 2
tandospirone
Lead
neuroleptic receptor
Proton Magnetic Resonance Spectroscopy

All Science Journal Classification (ASJC) codes

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

Cite this

Conformational analysis of tandospirone in aqueous solution : Lead evolution of potent dopamine D4 receptor ligands. / Nishimura, Tamiki; Igarashi, Jun etsu; Sunagawa, Makoto.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 9, 07.05.2001, p. 1141-1144.

Research output: Contribution to journalArticle

@article{f7790159485b4a71bd9a3b8b64f737a9,
title = "Conformational analysis of tandospirone in aqueous solution: Lead evolution of potent dopamine D4 receptor ligands",
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.",
author = "Tamiki Nishimura and Igarashi, {Jun etsu} and Makoto Sunagawa",
year = "2001",
month = "5",
day = "7",
doi = "10.1016/S0960-894X(01)00167-6",
language = "English",
volume = "11",
pages = "1141--1144",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "9",

}

TY - JOUR

T1 - Conformational analysis of tandospirone in aqueous solution

T2 - Lead evolution of potent dopamine D4 receptor ligands

AU - Nishimura, Tamiki

AU - Igarashi, Jun etsu

AU - Sunagawa, Makoto

PY - 2001/5/7

Y1 - 2001/5/7

N2 - 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.

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.

UR - http://www.scopus.com/inward/record.url?scp=0035821380&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035821380&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(01)00167-6

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

M3 - Article

C2 - 11354362

AN - SCOPUS:0035821380

VL - 11

SP - 1141

EP - 1144

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 9

ER -