Abstract
Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 495-500 |
| Number of pages | 6 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 11 |
| Issue number | 4 |
| DOIs | |
| State | Published - Feb 26 2001 |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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Cite this
Sakamuri, S., Enyedy, I. J., Kozikowski, A. P., Zaman, W. A., Johnson, K. M., & Wang, S. (2001). Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. Bioorganic and Medicinal Chemistry Letters, 11(4), 495-500. https://doi.org/10.1016/S0960-894X(00)00703-4