ABCA1和SR-B1双重基因上调表达剂5242331的合成  

Synthesis of ABCA1 and SR-B1 Dual Expression Upregulator 5242331

作　　者：田文华 姜珊 许艳妮 李文燕[1] TIAN Wenhua;JIANG Shan;XU Yanni;LI Wenyan(College of Chemistry and Materials Science,Hebei Normal University,Hebei Shijiazhuang 050024,China;National Center for Drug(Microbiology)Screening Laboratory,Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences,Beijing 100050,China)

机构地区：[1]河北师范大学化学与材料科学学院,河北石家庄050024 [2]中国医学科学院医药生物技术研究所,国家新药(微生物)筛选实验室,北京100050

出　　处：《河北师范大学学报（自然科学版）》2021年第6期603-606,共4页Journal of Hebei Normal University：Natural Science

基　　金：河北省自然科学基金京津冀基础研究合作专项(19JCZDJC63900)。

摘　　要：苯并噻唑类化合物5242331是通过高通量筛选得到的小分子ABCA1和SR-B1双重基因上调表达剂,具有较好的抗动脉粥样硬化作用.以4-正丁基苯胺为原料,环合得到2-氨基-6-丁基苯并噻唑中间体1,3-氨基丙腈与4-氯磺酰基苯甲酸酰化得到4-[(N-氰乙基)氨磺酰基]苯甲酸中间体2,再与中间体1缩合合成了化合物5242331,收率为71.6%.Benzothiazole 5242331 is an ABCA1 and SR-B1 dual expression upregulator obtained through high-throughput screening,which has a good anti-atherosclerosis effect.In this paper,2-amino-6-butyl benzothiazole intermediate 1 was synthesized from The 4-n-butylaniline by cyclization.The 4-(N-(2-cyanoethyl)sulfamoyl)benzoic acid intermediate 2 was obtained by acylation 3-aminopropionitrile with 4-(chlorosulfonyl)benzoic acid.The target compound 5242331 was get by condensation of intermediates 1 and 2 in a yield of 71.6%.

关 键 词：5242331 ABCA1 SR-B1 双重基因上调表达剂 合成 

分 类 号：R938.8[医药卫生—生药学]