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) |
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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 |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. / Sakamuri, Sukumar; Enyedy, Istvan J.; Kozikowski, Alan P.; Zaman, Wahiduz A.; Johnson, Kenneth M.; Wang, Shaomeng.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 4, 26.02.2001, p. 495-500.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors
AU - Sakamuri, Sukumar
AU - Enyedy, Istvan J.
AU - Kozikowski, Alan P.
AU - Zaman, Wahiduz A.
AU - Johnson, Kenneth M.
AU - Wang, Shaomeng
PY - 2001/2/26
Y1 - 2001/2/26
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0035952218&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0035952218&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(00)00703-4
DO - 10.1016/S0960-894X(00)00703-4
M3 - Article
C2 - 11229756
AN - SCOPUS:0035952218
VL - 11
SP - 495
EP - 500
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 4
ER -