One Pot Synthesis and Biological Activity Evaluation of Novel Schiff Bases Derived from 2-Hydrazinyl-1,3,4-thiadiazole

被引：31

作者：

Tehrani, Kamaleddin Haj Mohammad Ebrahim ^{[1
]}

Sardari, Soroush ^{[3
]}

Mashayekhi, Vida ^{[1
]}

Zadeh, Marjan Esfahani ^{[1
]}

Azerang, Parisa ^{[3
]}

Kobarfard, Farzad ^{[1
,2
]}

机构：

[1] Shahid Beheshti Univ Med Sci, Dept Med Chem, Sch Pharm, Tehran, Iran

[2] Shahid Beheshti Univ Med Sci, Phytochem Res Ctr, Tehran, Iran

[3] Inst Pasteur, Drug Design & Bioinformat Unit, Dept Med Biotechnol, Biotechnol Res Ctr, Tehran 13164, Iran

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2013年 / 61卷 / 02期

关键词：

1,3,4-thiadiazole-2-yl hydrazone; antiplatelet aggregation; thiosemicarbazone; antimycobacterial; MYCOBACTERIUM-TUBERCULOSIS; ANTIPLATELET THERAPY; DERIVATIVES; THIACETAZONE; INHIBITORS; AGGREGATION; ACTIVATION; MICE;

D O I：

10.1248/cpb.c12-00651

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Considering the structural features of a group of known potent inhibitors of human platelet aggregation containing hydrazone structural backbone, a series of novel hydrazone derivatives of 2-hydrazinyl-1,3,4-thiadiazole were synthesized using a one-pot process and tested for their inhibitory activity against platelet aggregation induced by arachidonic acid and ADP. Among the derivatives, compounds 3l, 3o and 3p exhibited the highest antiplatelet aggregation activity. The derivatives were also screened for their potential antimycobacterial activity and compounds 3g, 3k, 3p and 3q were among the most active compounds.

引用

页码：160 / 166

页数：7

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