具有噻唑苯磺酰胺药效基团的强效、选择性3-吡啶乙醇胺β3肾上腺素能受体激动剂。
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
作者信息
Mathvink R J, Tolman J S, Chitty D, Candelore M R, Cascieri M A, Colwell L F, Deng L, Feeney W P, Forrest M J, Hom G J, MacIntyre D E, Tota L, Wyvratt M J, Fisher M H, Weber A E
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2000 Sep 4;10(17):1971-3. doi: 10.1016/s0960-894x(00)00390-5.
A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. Incorporation of aryl and heteroaryl substitution in the 4-position of the thiazole ring resulted in a number of highly potent and selective beta3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described.
制备了一系列噻唑苯磺酰胺取代的3-吡啶基乙醇胺，并对其人类β3肾上腺素能受体激动剂活性进行了评估。在噻唑环的4-位引入芳基和杂芳基取代基，得到了许多高效且选择性的β3激动剂。描述了其中几种化合物的初步体内评估结果。
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