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Elsevier, Bioorganic and Medicinal Chemistry Letters, 2(24), p. 674-678, 2014

DOI: 10.1016/j.bmcl.2013.11.049

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Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors

Journal article published in 2013 by Zhuang Jin, Pasha Khan, Youseung Shin, Jingyi Wang, Li Lin, Michael D. Cameron ORCID, Jon M. Lindstrom, Paul J. Kenny, Theodore M. Kamenecka
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This paper is available in a repository.

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Abstract

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.