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
Hauptverfasser: Enyedy, Istvan J, Wang, Jiansuo, Zaman, Wahiduz A, Johnson, Kenneth M, Wang, Shaomeng
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Sprache:eng
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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).
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00243-3