SARs at the Monoamine Transporters for a Novel Series of Modafinil Analogues
| Autor: | Jonathan L. Katz, Jianjing Cao, Oluyomi M. Okunola, Thomas E. Prisinzano, Matthew Shook, Theresa A. Kopajtic, Amy Hauck Newman |
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| Rok vydání: | 2010 |
| Předmět: |
biology
business.industry Organic Chemistry Modafinil Sulfoxide Transporter Pharmacology Biochemistry chemistry.chemical_compound Monoamine neurotransmitter chemistry Norepinephrine transporter Amide Drug Discovery biology.protein Medicine business Serotonin transporter medicine.drug Dopamine transporter |
| Zdroj: | ACS Medicinal Chemistry Letters. 2:48-52 |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/ml1002025 |
| Popis: | A series of modafinil (1) analogues were synthesized wherein (1) para-halo-substitutents were added to the aryl rings, (2) the sulfoxide function was removed, and (3) the primary amide group was replaced with secondary and tertiary amides and amines to investigate the effects of these chemical modifications on dopamine transporter, serotonin transporter, and norepinephrine transporter binding. In addition, the locomotor-stimulant effects in mice of (±)-modafinil (1), its R- and S-enantiomers, and its para-chloro sulfinylacetamide analogue (5c) were compared to those of cocaine. |
| Databáze: | OpenAIRE |
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