Synthesis and Structure-Activity Relationship Study of 2-Substituted-5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles as Anti-Helicobacter pylori Agents

被引：4

作者：

Foroumadi, Alireza ^{[1
,2
,3
,4
]}

Sedaghat, Somayeh ^{[3
,4
]}

Emami, Saeed ^{[5
,6
]}

Yazdanian, Maryam ^{[3
,4
]}

Moshafi, Mohammad Hassan ^{[3
,4
]}

Safavi, Maliheh ^{[1
,2
]}

Sakhteman, Amirhossein ^{[1
,2
,7
]}

Firoozpour, Loghman ^{[1
,2
,7
]}

Vosooghi, Mohsen ^{[1
,2
]}

Shafiee, Abbas ^{[1
,2
,7
]}

机构：

[1] Univ Tehran Med Sci, Dept Med Chem, Fac Pharm, Tehran 14174, Iran

[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran

[3] Kerman Univ Med Sci, Dept Microbiol, Fac Pharm, Kerman, Iran

[4] Kerman Univ Med Sci, Kerman Neurosci Res Ctr, Kerman, Iran

[5] Mazandaran Univ Med Sci, Dept Med Chem, Sari, Iran

[6] Mazandaran Univ Med Sci, Pharmaceut Sci Res Ctr, Fac Pharm, Sari, Iran

[7] Univ Tehran Med Sci, Drug Design & Dev Res Ctr, Tehran 14174, Iran

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2009年 / 6卷 / 06期

基金：

美国国家科学基金会;

关键词：

Antibacterial activity; Anti-Helicobacter pylori activity; 1,3,4-Thiadiazole; Nitrothiophene; VITRO ANTIBACTERIAL ACTIVITY; QUINOLONE DERIVATIVES; RESISTANCE; CLARITHROMYCIN; LEVOFLOXACIN; ERADICATION; FLUOROQUINOLONES; AMOXICILLIN; THERAPY;

D O I：

10.2174/157018009789057599

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some alkylthio, alkylsulfinyl and alkylsulfonyl-5-(5-nitro-2-thienyl)-1,3,4-thiadiazoles were synthesized and evaluated against Helicobacter pylori. The antibacterial data indicated that most compounds exhibited significant inhibitory activity against H. pylori-more potent than standard drug metronidazole. Among them, 2-ethylsulfinyl-5-(5-nitro-2thienyl)-1,3,4-thiadiazole was the most potent compound tested against clinical isolates of H. pylori. Generally the SAR of this series of compounds indicated that both the structure of the alkyl pendent and the S, SO or SO2 linker dramatically impact the antibacterial activity against H. pylori.

引用

页码：468 / 474

页数：7

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