Discovery of substituted 3,4-Diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol
Substituted 3,4-diphenyl-1,3-thiazols were identified as a class of novel and potent monoamine transporter inhibitors through a 3-D pharmacophore search using a new pharmacophore model derived from mazindol. The most potent compound ( 13) has K i values of 24 and 23 nM in binding to dopamine transpo...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2002-07, Vol.12 (13), p.1775-1778 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | Substituted 3,4-diphenyl-1,3-thiazols were identified as a class of novel and potent monoamine transporter inhibitors through a 3-D pharmacophore search using a new pharmacophore model derived from mazindol. The most potent compound (
13) has
K
i values of 24 and 23
nM in binding to dopamine transporter and inhibition of dopamine reuptake, respectively.
3,4-Diphenyl-thiazoles were identified as a novel class of monoamine transporter inhibitors (
K
i=24
nM at DAT). |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(02)00243-3 |