Seyed.Esmaeil Sadat Eebrahimi , Maryam Mirmohammadi , Zahra Mojallal Tabatabaei , Marjan Azimzadeh Arani , Sogol Jafari Ashtiani , Mahsa Hashemian , Parham Foroumadi , Azadeh Yahya Meymandi , Setareh Moghimi , Mohammad Hasan Moshafi , Peiman Norouzi , Sussan Kabudanian Ardestani , Alireza Foroumadi *
In this study, a series of novel compounds based on 5-(5-nitrothiophene-2-yl)-1,3,4-thiadiazole possessing (het)aryl thio pendant at C-2 position of thiadiazole ring is developed and evaluated as antileishmanial agents using MTT colorimetric assay. 10 New compounds containing aryl and hetero aryl derivatives, started from thiophene-2-carbaldehyde in five steps, were synthesized in good to excellent yields and characterized by 1H-NMR, 13C-NMR and IR spectroscopy. Through the compounds 6a-j, methylimidazole containing derivative 6e was recognized as the most active compound against L. major promastigotes exhibiting IC50 values of 11.2µg/ml and 7.1µg/ml after 24 and 48 hours, respectively. This compound is >4 fold more effective than Glucantime as a standard drug (IC50 = 50 µg/ml after 24 h and 25 µg/ml after 48 h).
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