The design and synthesis of a series of substituted heteroaromatic alpha4beta2alpha5 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.
        
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Jin Z, Khan P, Shin Y, Wang J, Lin L, Cameron MD, Lindstrom JM, Kenny PJ, Kamenecka TM (2014) Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for alpha4beta2alpha5 nicotinic acetylcholine receptors Bioorganic & Medicinal Chemistry Lett24: 674-8
Jin Z, Khan P, Shin Y, Wang J, Lin L, Cameron MD, Lindstrom JM, Kenny PJ, Kamenecka TM (2014) Bioorganic & Medicinal Chemistry Lett24: 674-8