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).
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Tahghighi A,Emami S,Razmi S,Rezazade Marznaki F,Kabudanian Ardestani S,Dastmalchi S,Kobarfard F,Shafiee A,Foroumadi Adoi
10.3109/14756366.2012.689297subject
Has Abstractpub_date
2013-08-01 00:00:00pages
843-52issue
4eissn
1475-6366issn
1475-6374journal_volume
28pub_type
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