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  • Title: Synthesis and in vitro leishmanicidal activity of 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-substituted-1,3,4-thiadiazole derivatives.
    Author: Foroumadi A, Emami S, Pournourmohammadi S, Kharazmi A, Shafiee A.
    Journal: Eur J Med Chem; 2005 Dec; 40(12):1346-50. PubMed ID: 16095763.
    Abstract:
    A series of 2-(1-methyl-5-nitroimidazol-2-yl)-5-(1-piperazinyl, 1-piperidinyl and 1-morpholinyl)-1,3,4-thiadiazoles (3a-g) were synthesized and evaluated for in vitro leishmanicidal activity against Leishmania major promastigotes. The leishmanicidal data revealed that compounds 3a-g had strong and much better leishmanicidal activity than the reference drug pentostam. Compound 3c (piperazine analog) was the most active compound (IC50=0.19 microM).
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