78961-42-9Relevant articles and documents
Synthesis and Pharmacological Evaluation of Novel Pyrazolyl Piperidine Derivatives as Effective Antiplatelet Agents
Soni, Jigar Y.,Tamboli, Riyaj S.,Giridhar, Rajani,Yadav, Mange Ram,Thakore, Sonal
, p. 1279 - 1286 (2017/03/27)
The synthesis and antiplatelet activity of substituted pyrazolyl piperidine derivatives (3a–n) are described. These compounds were synthesized by an improved ring opening reaction of 2-arylidene quinuclidinone using hydrazine hydrate under mild conditions
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands
Mazurov, Anatoly,Klucik, Jozef,Miao, Lan,Phillips, Teresa Y.,Seamans, Angela,Schmitt, Jeffrey D.,Hauser, Terry A.,Johnson Jr., Raymond T.,Miller, Craig
, p. 2073 - 2077 (2007/10/03)
A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as α7 neuronal nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore model. The series is highly selective for the α7 over other nAChRs (e.g., the α4β2 of the CNS, and the muscle and ganglionic subtypes) and is functionally tunable at α7. One member of the series, (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan-2-carboxamide (+)-8l), has potent agonistic activity for the α7 nAChR (EC50 = 33 nM, Imax = 1.0), at concentrations below those that result in desensitization.