Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity was written by Couhert, Audrey;Delagrange, Philippe;Caignard, Daniel-Henri;Chartier, Agnes;Suzenet, Franck;Guillaumet, Gerald. And the article was included in European Journal of Medicinal Chemistry in 2016.Category: pyridine-derivatives This article mentions the following:
An efficient synthesis of 2-substituted furo[3,2-b]pyridines and their biol. evaluation as melatonin receptors ligands was reported. The proposed eight-step sequence ending with a Suzuki coupling allowed a rapid access to various analogs. The steric hindrance and the conformation of the aryl group in C2-position were evaluated regarding the selectivity of the mol. for one of the two high affinity melatonin receptors as well as the activity profile of the compound Introduction of 1-naphthyl substituent gave the best result in terms of selectivity with a MT1/MT2 ratio of about 150 (MT1 Ki = 198 nM, MT2 Ki = 1.3 nM). In the experiment, the researchers used many compounds, for example, 5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0Category: pyridine-derivatives).
5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Category: pyridine-derivatives