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Cocconcelli G.,Siena Biotech S.p.A. | Ghiron C.,Siena Biotech S.p.A. | Haydar S.,Chemical science and Neuroscience Discovery Research | Micco I.,Siena Biotech S.p.A. | Zanaletti R.,Siena Biotech S.p.A.
Synthetic Communications | Year: 2010

A new and efficient synthesis for the preparation of novel 4-fluoro-2H-pyrazol-3-ylamines is described. It involves the reaction of an acyl chloride with fluoroacetonitrile and sequential ring closure of the-fluoro-ketonitrile with hydrazine. Utilizing this synthetic protocol, we have synthesized a variety of 4-fluoro-2H-pyrazol-3-ylamines with different steric and electronic demands. © Taylor & Francis Group, LLC.

Ghiron C.,Siena Biotech S.p.A. | Haydar S.N.,Chemical science and Neuroscience Discovery Research | Aschmies S.,Chemical science and Neuroscience Discovery Research | Bothmann H.,Siena Biotech S.p.A. | And 26 more authors.
Journal of Medicinal Chemistry | Year: 2010

Alpha-7 nicotinic acetylcholine receptor (α7 nAChR) agonists are promising therapeutic candidates for the treatment of cognitive impairment. We report a series of novel, potent small molecule agonists (4-18) of the α7 nAChR deriving from our continuing efforts in the areas of Alzheimer's disease and schizophrenia. One of the compounds of the series containing a urea moiety (16) was further shown to be a selective agonist of the α7 nAChR with excellent in vitro and in vivo profiles, brain penetration, and oral bioavailability and demonstrated in vivo efficacy in multiple behavioral cognition models. Structural modifications leading to the improved selectivity profile and the biological evaluation of this series of compounds are discussed. © 2010 American Chemical Society.

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