Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Huang, Huoming, once mentioned the application of 41556-26-7, Name is Bis(1,2,2,6,6-pentamethylpiperidin-4-yl) decanedioate, molecular formula is C30H56N2O4, molecular weight is 508.78, MDL number is MFCD00134706, category is piperidines. Now introduce a scientific discovery about this category, Application In Synthesis of Bis(1,2,2,6,6-pentamethylpiperidin-4-yl) decanedioate.
Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxypheny1)-N-phenylpiperidine-1-carboxamide as novel potent analgesic
Management of moderate to severe pain by clinically used opioid analgesics is associated with a plethora of side effects. Despite many efforts have been dedicated to reduce undesirable side effects, moderate progress has been made. In this work, starting from Tramadol, a series of 3-((dimethylamino)methyl)-4hydroxy-4-(3-methoxyphenyl)piperidine-1-carboxamide derivatives were designed and synthesized, and their in vitro and in vivo activities were evaluated. Our campaign afforded selective opioid receptor (MOR) ligand 2a (K-i (MOR): 7.3 +/- 0.5 nM; K-iDOR: 849.4 +/- 96.6 nM; K-i KOR: 49.1 +/- 6.9 nM) as potent analgesic with ED50 of 3.1 mg/kg in 55 degrees C hot plate model. Its antinociception effect was blocked by opioid antagonist naloxone. High binding affinity toward MOR of compound 2a was associated with water bridge, salt bridge, hydrogen bond and hydrophobic interaction with MOR. The high selectivity of compound 2a for MOR over delta opioid receptor (DOR) and kappa opioid receptor (KOR) was due to steric hindrance of compound 2a with DOR and KOR. 2a, a compound with novel scaffold, could serve as a lead for the development of novel opioid ligands. (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem