1-芳基-3-烷基-1,4-二氢-4-取代-5H-1,2,4-三唑啉酮-5衍生物的合成及生物活性  

Synthesis and Bioactivity of 1-Aryl-3-Alkyl-1, 4-Dihydro-4-Substituted-5H-1,2,4-triazolinones-5

作　　者：徐进宜[1] 周宇昕[1] 吴晓明[1] 唐康[2] 王秋娟[2] 

机构地区：[1]中国药科大学药物化学教研室,南京210009 [2]中国药科大学生理学教研室,南京210009

出　　处：《中国药科大学学报》1999年第5期332-337,共6页Journal of China Pharmaceutical University

摘　　要：为寻找新的高效非肽类血管紧张素Ⅱ（AⅡ）受体括抗剂,以SC-51316为先导,运用生物电子等排和拼合原理,设计并合成了9个1-芳基-3-烷基-1,4-二氢-4-取代-5H-1,2,4-三唑啉酮-5衍生物。所有目的化合物均未见文献报道,其结构经IR、1HNMR和MS鉴定。初步体外药理实验表明：在抑制AⅡ诱发的兔主动脉收缩反应模型中,化合物17h具有较好的活性。In order to search for the new nonpeptide A Ⅱ receptor antagonists with high Potency, Using SC-51316 as a lead compound, and based on the principles of bioisosterism and hybridization, a series of 1-aryl-3-alkyl-1, 4-dihydro-4-substituted-5 H-1, 2, 4-triazolinones-5 are designed and synthesized. All the target compounds are unreported and identified by IR, lHNMR and MS spectrum, in vitro pharmacological test, compound 17 h exhibits certuin potency of inhibiting A Ⅱ-mediated contraction of rabbit aortic ring.

关 键 词：AT1受体拮抗剂 三唑啉酮 合成 降压药 

分 类 号：TQ463.54[化学工程—制药化工]