Synthetic Route of 108-26-9, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 108-26-9, Name is 3-Methyl-1H-pyrazol-5(4H)-one, SMILES is O=C1CC(C)=NN1, belongs to piperidines compound. In a article, author is Zhang, Han, introduce new discover of the category.
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as alpha 7 nicotinic receptor antagonists
alpha: 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 alpha 7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective alpha 7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761-0184 that acts as a alpha 7 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 alpha 7 with their IC50 values ranging from 3.3 mu M to 13.7 mu M. Compound B10 exhibited alpha 7 selectivity over other alpha 4 beta 2 and alpha 3 beta 4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective alpha 7 nAChR antagonists. (C) 2020 Elsevier Masson SAS. All rights reserved.
Synthetic Route of 108-26-9, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 108-26-9.
Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem