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

Istvan J. Enyedy; Jiansuo Wang; Wahiduz A. Zaman; Kenneth M. Johnson; Shaomeng Wang

doi:10.1016/S0960-894X(02)00243-3

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

Istvan J. Enyedy, Jiansuo Wang, Wahiduz A. Zaman, Kenneth M. Johnson, Shaomeng Wang

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

14 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1775-1778
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	13
DOIs	https://doi.org/10.1016/S0960-894X(02)00243-3
State	Published - Jul 8 2002
Externally published	Yes

ASJC Scopus subject areas

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

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10.1016/S0960-894X(02)00243-3

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Enyedy, I. J., Wang, J., Zaman, W. A., Johnson, K. M., & Wang, S. (2002). 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. Bioorganic and Medicinal Chemistry Letters, 12(13), 1775-1778. https://doi.org/10.1016/S0960-894X(02)00243-3

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. / Enyedy, Istvan J.; Wang, Jiansuo; Zaman, Wahiduz A. et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 12, No. 13, 08.07.2002, p. 1775-1778.

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

Enyedy, IJ, Wang, J, Zaman, WA, Johnson, KM & Wang, S 2002, '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', Bioorganic and Medicinal Chemistry Letters, vol. 12, no. 13, pp. 1775-1778. https://doi.org/10.1016/S0960-894X(02)00243-3

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AU - Zaman, Wahiduz A.

AU - Johnson, Kenneth M.

AU - Wang, Shaomeng

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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

Abstract

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