Design and Synthesis of N-Aryl Isothioureas as a Novel Class of Gastric H+/K+-ATPase Inhibitors

被引：12

作者：

Ma, Chao ^{[1
]}

Wu, Anhui ^{[1
]}

Wu, Yongqi ^{[1
]}

Ren, Xuhong ^{[1
]}

Cheng, Maosheng ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct Based Drugs Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2013年 / 346卷 / 12期

关键词：

H+; K+-ATPase; N-Aryl isothiourea; Synthesis; PROTON PUMP INHIBITORS;

D O I：

10.1002/ardp.201300276

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To find new H+/K+-ATPase inhibitors for the treatment of peptic ulcer disease, a series of novel N-aryl isothiourea derivatives were synthesized and their structures were identified by H-1 NMR and GC-MS. The effects of these compounds on inhibiting gastric acid secretion were evaluated by the guinea pig stomach mucous membrane study with pantoprazole magnesium as a positive control. The results showed that, of the 37 N-aryl isothiourea compounds synthesized, 20 compounds have comparable or stronger gastric acid inhibitory activities than that of pantoprazole magnesium. The quantitative structure-activity relationships (QSARs) of the N-aryl isothiourea compounds were also studied by comparative molecular field analysis (CoMFA) computation, and the model structure that was supposed to give more powerful bioactivities was finally predicted.

引用

页码：891 / 900

页数：10

共 15 条

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[2]

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