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  • Title: New 5-(nitroheteroaryl)-1,3,4-thiadiazols containing acyclic amines at C-2: synthesis and SAR study for their antileishmanial activity.
    Author: Tahghighi A, Emami S, Razmi S, Rezazade Marznaki F, Kabudanian Ardestani S, Dastmalchi S, Kobarfard F, Shafiee A, Foroumadi A.
    Journal: J Enzyme Inhib Med Chem; 2013 Aug; 28(4):843-52. PubMed ID: 22651800.
    Abstract:
    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 >12).
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