41661-56-7Relevant academic research and scientific papers
Very Strong and Selective Complexation of Small Metal Ions by a Highly Preorganised Open-chain Bispidine-based Ligand
Hosken, Gladys D.,Hancock, Robert D.
, p. 1363 - 1364 (1994)
Synthesis of 3,7-bis(2-pyridylmethyl)-3,7-diazabicyclononane DPB, with very rigid nitrogen-bridge reinforcement gives an adamantane-like structure once a metal ion is coordinated to DPB, and shows how remarkable stability enhancement and selectivity for metal ions on the basis of size can be achieved in non-macrocyclic ligands.
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists
Zhang, Han,He, Xiaomeng,Wang, Xintong,Yu, Bo,Zhao, Siqi,Jiao, Peili,Jin, Hongwei,Liu, Zhenming,Wang, KeWei,Zhang, Liangren,Zhang, Lihe
, (2020/09/03)
α: 7 nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems have been suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761–0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3 μM to 13.7 μM. Compound B10 exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.
Development of a manufacturing process for 1-(1-pyridin-2-yl methyl-piperidin-4-yl)-1H-indole: A key intermediate for protein kinase C inhibitor LY317615
Boini, Sathish,Moder, Kenneth P.,Vaid, Radhe K.,Kopach, Micheal,Kobierski
, p. 1205 - 1211 (2012/12/23)
This contribution describes process development leading to the production of 1-(1-pyridin-2-yl methyl-piperidin-4-yl)-1H-indole (11). The title compound 11 was produced via a Leimgruber-Batcho indole synthesis using key intermediates 2-(2,2-dimethoxyethyl
Green chemistry approach to the synthesis of N-substituted piperidones
Faul, Margaret M.,Kobierski, Michael E.,Kopach, Michael E.
, p. 5739 - 5741 (2007/10/03)
An efficient green chemistry approach to the synthesis of N-substituted piperidones and piperidines was developed and applied to the synthesis of 1-(2-pyridinylmethyl)-piperidin-4-one, 1, a key starting material for the synthesis of LY317615, an antiangio
Strategies for the synthesis of N-(azacycloalkyl)bisindolylmaleimides: Selective inhibitors of PKCβ
Faul, Margaret M.,Grutsch, John L.,Kobierski, Michael E.,Kopach, Michael E.,Krumrich, Christine A.,Staszak, Michael A.,Udodong, Uko,Vicenzi, Jeffrey T.,Sullivan, Kevin A.
, p. 7215 - 7229 (2007/10/03)
N-(Azacycloalkyl)bisindolylmaleimides 1 have been identified to be selective inhibitors of PKCβ. This manuscript will describe the synthetic approaches employed to prepare this class of compounds that resulted in development of efficient methods for prepa
