Abreo, Melwyn A.; Lin, Nan-Horng; Garvey, David S.; Gunn, David E.; Hettinger, Anne-Marie; Wasicak, James T.; Pavlik, Patricia A.; Martin, Yvonne C.; Donnelly-Roberts, Diana L. published the article 《Novel 3-Pyridyl Ethers with Subnanomolar Affinity for Central Neuronal Nicotinic Acetylcholine Receptors》. Keywords: pyridinyl ether preparation nicotinic acetylcholine receptor; nicotininc cholinergic receptor azedidinylmethoxy pyrrolidinylmethoxy pyridine.They researched the compound: Boc-D-Prolinol( cas:83435-58-9 ).Quality Control of Boc-D-Prolinol. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:83435-58-9) here.
Recent evidence indicating the therapeutic potential of cholinergic channel modulators for the treatment of central nervous system (CNS) disorders as well as the diversity of brain neuronal nicotinic acetylcholine receptors (nAChRs) have suggested an opportunity to develop subtype-selective nAChR ligands for the treatment of specific CNS disorders with reduced side effect liabilities. The synthesis of a novel series of 3-pyridyl ether compounds was reported which possess subnanomolar affinity for brain nAChRs and differentially activate subtypes of neuronal nAChRs. The synthesis and structure-activity relationships for the leading members of the series are described, including A-85380, which possesses ca. 50 pM affinity for rat brain [3H]-(-)-cytisine binding sites and 163% efficacy compared to nicotine to stimulate ion flux at human α4β2 nAChR subtype, and A-84543, which exhibits 84-fold selectivity to stimulate ion flux at human α4β2 nAChR subtype compared to human ganglionic type nAChRs. Computational studies indicate that a reasonable superposition of a low energy conformer of A-85380 with (S)-nicotine and (-)-epibatidine can be achieved. An example compound are (S)-3-[(1-methyl-2-pyrrolidinyl)methoxy]pyridine and (S)-3-(1-methyl-2-azetidinylmethoxy)pyridine.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica