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- Title
Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major.
- Authors
Sadat-Ebrahimi, Seyed Esmail; Mirmohammadi, Maryam; Tabatabaei, Zahra Mojallal; Arani, Marjan Azimzadeh; Jafari-Ashtiani, Sogol; Hashemian, Mahsa; Foroumadi, Parham; Yahya-Meymandi, Azadeh; Moghimi, Setareh; Moshafi, Mohammad Hassan; Norouzi, Peiman; Ardestani, Susan Kabudanian; Foroumadi, Alireza
- Abstract
In this study, a series of novel compounds based on 5-(5-nitrothiophene2--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 heteroaryl 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 h, 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).
- Subjects
LEISHMANIA major; THIADIAZOLES; LEISHMANIA mexicana; AROMATIC compounds; LEISHMANIA; DRUG standards
- Publication
Iranian Journal of Pharmaceutical Research, 2019, Vol 18, Issue 4, p1816
- ISSN
1735-0328
- Publication type
Article
- DOI
10.22037/ijpr.2019.14547.12476