作者:刘文超1;,张晓楠1;,许龙1;,张新1;,秦华2;,朱长进1;,马兵1; (1北京理工大学化学与化工学院;2北京天衡军威医药技术开发有限公司)
出处:沈阳药科大学学报 2023
关键词:醛糖还原酶抑制剂;糖尿病并发症;分子对接
摘要:目的 设计合成一系列靛红衍生物,研究其对醛糖还原酶的抑制活性和选择性。方法 以5-溴靛红为起始原料合成5′-溴螺[[1,3]二氧戊环-2,3′-吲哚啉]-2′-酮的三环骨架,然后经N烷基化反应、Suzuki或Heck偶联、水解合成了目标化合物。测定目标化合物对醛糖还原酶的抑制活性和选择性,通过计算机 ...
作者:Zhongfei Han;Jiahui Li;Zilu Xu;Yu Su;Yihan Wang;Lili Zhuo;Jiaming Du;Changjin Zhu;Xin Hao (1 Faculty of Chemistry and Chemical Engineering, Yancheng Institute of Technology, Yancheng, China. 2 Department of Applied Chemistry, Beijing Institute of Technology, Beijing, China.)
出处:Archiv der Pharmazie 2023
关键词:AKR1B1 inhibitor;diabetic complications;quinazolin-4(1H)-one.
摘要:Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecu ...
作者:Zhu, Junkai;Qi, Gang;Kuang, Yan;Zhao, Yating;Sun, Xinjie;Zhu, Changjin;Hao, Xin;Han, Zhongfei (1Faculty of Chemistry and Chemical Engineering, Yancheng Institute of Technology, Yancheng, China;2Department of Applied Chemistry, Beijing Institute of Technology, Beijing, China)
出处:Archiv der Pharmazie 2022
关键词:Complicações do Diabetes;Diabetes Mellitus;Aldeído Redutase;Aminas;Benzilaminas;Ácidos Carboxílicos;Inibidores Enzimáticos/química;Inibidores Enzimáticos/farmacologia;Humanos;Simulação de Acoplamento Molecular;Relação Estrutura-Atividade
摘要:A series of 9H-purin-6-amine derivatives as aldose reductase (ALR) inhibitors were designed and synthesized. Most of these derivatives, having a C6-su ...
发明人:朱长进,马兵,张新
申请日期:2020.12.08
摘要:本发明公开了一系列苯并噁唑酮类衍生物的结构、制备方法及用途,即提供了化合物Ⅰ所示苯并噁唑酮类化合物结构、合成方法、及其药学上可以接受的盐或它们的混合物在制备预防和/或治疗糖尿病并发症药物中的用途。这类化合物作为醛糖还原酶抑制剂和抗氧化剂,还具有降血糖效果。该类化合物可以降血糖,抑制醛糖还原酶的活性, ...