期刊
JOURNAL OF NATURAL PRODUCTS
卷 78, 期 4, 页码 722-729出版社
AMER CHEMICAL SOC
DOI: 10.1021/np500893h
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资金
- U.S. National Institutes of Health (NIH) [1SC-1GM092282, G12RR003037]
- National Institute of Mental Health's (NIMH) Psychoactive Drug Screening Program [HHSN-271-2008-00025-C]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [1228921] Funding Source: National Science Foundation
N-Methyllaurotetanine (1) has been reported to display good affinity for the 5-HT1A receptor, but no structureaffinity studies have been performed to date. The commercially available alkaloid boldine (2) was used as the starting material for synthesis of various C-9 alkoxy analogues of N-methyllaurotetanine in order to gauge the effect of C-9 alkylation on affinity and selectivity at 5-HT1A, 5-HT2A, and 5-HT7 receptors. Mitsunobu reactions were implemented in the alkylation steps leading to the analogues. Modest improvement in 5-HT1A affinity was observed upon alkylation for most analogues. Thus, the C-9 hydroxy group of 1 is not critical for affinity to the 5-HT1A receptor. Some analogues displayed high affinity for the 5-HT7 receptor, comparable to N-methyllaurotetanine, with moderate selectivity vs 5-HT1A and 5-HT2A receptors.
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