Safety of Ethyl indoline-2-carboxylate. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Ethyl indoline-2-carboxylate, is researched, Molecular C11H13NO2, CAS is 50501-07-0, about α2-Adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines. Author is Hlasta, Dennis J.; Luttinger, Daniel; Perrone, Mark H.; Silbernagel, Marla J.; Ward, Susan J.; Haubrich, Dean R..
The synthesis and α2-adrenergic activity of a series of indolin-2-yl- and tetrahydroquinolin-2-ylimidazolines, e.g. I (R = Me, Et, allyl, Ph, CH2Ph, etc.; R1 = 5-F, 5-Cl, etc.) and II (R = H, Me) are described. The indolin-2-ylimidazoline I (R = Me, R1 = H) has potent α2-adrenergic agonist and antagonist activity. The modification of the substituents on the indoline ring of I led to the separation of these activities. Substitution on the aromatic ring of I with halogen or increasing the size of the N-alkyl substituent of I gave α2-adrenergic antagonists without agonist activity. The N-allylindoline I (R = allyl, R1 = H) is more potent than idazoxan in vitro and is equipotent in vivo, but is less receptor-selective (α2 vs. α1) than idazoxan. cis-1,3-Dimethylindolin-2-ylimidazoline is an α2-adrenergic agonist equal in potency to clonidine in vitro, whereas trans-1,3-dimethylindolin-2-ylimidazoline is a moderately potent α2-adrenergic antagonist.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics