Related Products of 1690-72-8On October 31, 1990 ,《Synthesis and biological activity of 1,2,4-oxadiazole derivatives: highly potent and efficacious agonists for cortical muscarinic receptors》 appeared in Journal of Medicinal Chemistry. The author of the article were Street, Leslie J.; Baker, Raymond; Book, Tracey; Kneen, Clare O.; MacLeod, Angus M.; Merchant, Kevin J.; Showell, Graham A.; Saunders, John; Herbert, Richard H.. The article conveys some information:
The synthesis and biochem. evaluation of novel 1,2,4-oxadiazole-based muscarinic agonists which can readily penetrate into the CNS is reported. Efficacy and binding of these compounds are markedly influenced by the structure and physicochem. properties of the cationic head group. In a series of azabicyclic ligands efficacy and affinity are influenced by the size of the surface area presented to the receptor at the active site, and the degree of conformational flexibility. The exo-1-azanorbornane I represents the optimum arrangement, and this compound is one of the most efficacious and potent muscarinic agonists known. In a series of isoquinuclidine-based muscarinic agonists efficacy and affinity are influenced by the geometry between the cationic head group and H-bond acceptor pharmacophore and steric bulk in the vicinity of the base. The anti configuration represented by II is optimal for muscarinic activity. Ligands with pKa <6.5 show poor binding to the muscarinic receptor as exemplified by the diazabicyclic derivative III. In the experiment, the researchers used Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8Related Products of 1690-72-8)
Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 1690-72-8
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem