Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands
Citations Over Time
Abstract
The effect of variation of the 1-azabicyclic substituent on the novel 1,2,3-triazol-4-yl-, 1,2,4-triazol-1-yl, tetrazol-5-yl-, and tetrazol-2-yl-based muscarinic receptor ligands has been studied, and the exo-azabicyclic[2.2.1]hept-3-yl substituent was found to give the most potent and efficacious compounds. In addition, variation of the second substituent on 1,2,4-triazol-1-yl- and tetrazol-2-yl-based muscarinic receptor ligands has yielded a series of novel compounds with high potencies and efficacies, ranging from full agonists to antagonists. Small lipophilic electron withdrawing substituents give potent but low efficacy compounds, while small polar electron donating substituents give potent and efficacious compounds. The activity of these compounds is described in terms of a model of the receptor involving lipophilic and hydrogen bonding interactions. These compounds provide muscarinic ligands with high potency and a range of efficacies suitable for testing as candidate drugs in the treatment of Alzheimer's disease.
Related Papers
- → Novel polyoxometalate-based cobalt complexes based on rigid pyridyl-triazole-tetrazole and pyridyl-bis(triazole) ligands(2018)18 cited
- → Combining the most suitable energetic tetrazole and triazole moieties: synthesis and characterization of 5-(1-hydroxy-3-nitro-1,2,4-triazol-5-yl)-1-hydroxy-tetrazole and its nitrogen-rich ionic derivatives(2022)14 cited
- → Synthesis of Polymers Including Both Triazole and Tetrazole by Click Reaction(2011)17 cited
- → Synthesis of azo compounds containing triazole and tetrazole residues(1974)14 cited