知识与财富的链接
结合苯基哌基类α_1-受体拮抗剂的构效关系和我们应用计算机辅助药物设计 方法所构建的药效团模型,设计并合成了呋喃-2-甲酸{ω-[4-（取代苯基）-1-哌 嗪基]-烷基}酰胺和2-氧代-2H-苯并吡喃-3-羧酸{ω-[4-（取代苯基）-1-哌嗪基]- 烷基}酰胺两类衍生物,其结构经~1H NMR,IR及MS（HRMS）确证。初步生物活性测 试表明,所合成的目标化合物多数具有较好的α_1-受体拮抗剂,良性前列腺增生 。
Novel furan-2-carboxylic acid {ω-[4-(substituted phenyl)- piperazine-1-yl]alkyl} amide and 2-oxo-2H-chromene-3-carboxylic acid {ω -[4-(substituted phenyl)-piperazine-1-yl]alkyl} amide derivatives have been designed and synthesized based on the structure and acitivity relationship (SAR) of phenylpiperazine series as α_1-adrenoceptor (α _1-AR) antagonists and the results of computer-aided drug design we studied before. All the target compounds have been identified by ~1H NMR, IR and MS (HRMS). Preliminary bioassay suggests that most of the target compounds display good blocking activity to α_1-AR. The potency (pA_2) of compound 3b is higher than prazosin.
