Romeo Giuseppe, Materia Luisa, Marucci Gabriella, Modica Maria, Pittalà Valeria, Salerno Loredana, Siracusa Maria Angela, Buccioni Michela, Angeli Piero, Minneman Kenneth P
Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy.
Bioorg Med Chem Lett. 2006 Dec 15;16(24):6200-3. doi: 10.1016/j.bmcl.2006.09.034. Epub 2006 Oct 5.
A number of new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives were synthesized and evaluated for their binding and functional properties at alpha(1)-adrenergic receptor (alpha(1)-AR) subtypes. They behaved as potent alpha(1)-AR antagonists. In binding experiments, some of them (RC24 and RC23) showed very high affinity for the alpha(1D)-AR subtype.
合成了一系列新的嘧啶并[5,4 - b]吲哚和[1]苯并噻吩并[3,2 - d]嘧啶衍生物，并对它们在α(1) - 肾上腺素能受体（α(1) - AR）亚型上的结合和功能特性进行了评估。它们表现为强效的α(1) - AR拮抗剂。在结合实验中，其中一些（RC24和RC23）对α(1D) - AR亚型显示出非常高的亲和力。
