Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors
The design and synthesis of a series of substituted heteroaromatic α4β2α5 positive allosteric modulators is reported. The optimization and development of the heteroaromatic series was carried out from NS9283, and several potent analogues, such as 3-(5-(pyridin-3-yl)-2H-tetrazol-2-yl)benzonitrile (5k...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2014-01, Vol.24 (2), p.674-678 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Jin, Zhuang Khan, Pasha Shin, Youseung Wang, Jingyi Lin, Li Cameron, Michael D. Lindstrom, Jon M. Kenny, Paul J. Kamenecka, Theodore M. |
| description | The design and synthesis of a series of substituted heteroaromatic α4β2α5 positive allosteric modulators is reported. The optimization and development of the heteroaromatic series was carried out from NS9283, and several potent analogues, such as 3-(5-(pyridin-3-yl)-2H-tetrazol-2-yl)benzonitrile (5k) and 3,3′-(2H-tetrazole-2,5-diyl)dipyridine (12h) with good in vitro efficacy were discovered. |
| doi_str_mv | 10.1016/j.bmcl.2013.11.049 |
| format | Article |
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All rights reserved. 2013</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3709-d487b9ceb039fdba7bb6228b75218fb8a6ecd7bbc3eedee87baee547931f99343</citedby><cites>FETCH-LOGICAL-c3709-d487b9ceb039fdba7bb6228b75218fb8a6ecd7bbc3eedee87baee547931f99343</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X13013401$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24365158$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jin, Zhuang</creatorcontrib><creatorcontrib>Khan, Pasha</creatorcontrib><creatorcontrib>Shin, Youseung</creatorcontrib><creatorcontrib>Wang, Jingyi</creatorcontrib><creatorcontrib>Lin, Li</creatorcontrib><creatorcontrib>Cameron, Michael D.</creatorcontrib><creatorcontrib>Lindstrom, Jon M.</creatorcontrib><creatorcontrib>Kenny, Paul J.</creatorcontrib><creatorcontrib>Kamenecka, Theodore M.</creatorcontrib><title>Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>The design and synthesis of a series of substituted heteroaromatic α4β2α5 positive allosteric modulators is reported. 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| ispartof | Bioorganic & medicinal chemistry letters, 2014-01, Vol.24 (2), p.674-678 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Allosteric Regulation - drug effects Allosteric Regulation - physiology Animals HEK293 Cells Humans Mice Nicotinic Agonists - chemical synthesis Nicotinic Agonists - pharmacology Nicotinic Antagonists - chemical synthesis Nicotinic Antagonists - pharmacology Oxadiazoles - chemical synthesis Oxadiazoles - pharmacology Positive allosteric modulators Pyridines - chemical synthesis Pyridines - pharmacology Receptors, Nicotinic - physiology Structure-Activity Relationship Substituted heteroaromatics α4β2α5 |
| title | Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors |
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