New 5-(nitroheteroaryl)-1,3,4-thiadiazols containing acyclic amines at C-2: synthesis and SAR study for their antileishmanial activity

作者：Tahghighi Azar; Emami Saeed; Razmi Sepide; Marznaki Farzane Rezazade; Ardestani Sussan Kabudanian; Dastmalchi Siavoush; Kobarfard Farzad; Shafiee Abbas; Foroumadi Alireza^*

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2013, 28(4): 843-852.

DOI：10.3109/14756366.2012.689297

• Antileishmanial activity
• 5-nitrofuran
• 5-nitrothiophene
• 1,3,4-thiadiazole

A novel series of 5-(5-nitrofuran-2-yl)-and 5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazole-2-amines bearing acyclic amine at C-2 position of thiadiazole ring were synthesized and evaluated in vitro against promastigote and amastigote forms of Leishmania major. The structure-activity of series was investigated by studying 40 compounds. The most active derivatives were hydroxypropylamino-and methoxypropylamino-analogs of 5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazole (compounds 29 and 32, respectively) with highest selectivity index (SI %26gt; 12).

• 出版日期2013-8