Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major
| Author | Seyed Esmail Sadat-Ebrahimi | en |
| Author | Maryam Mirmohammadi | en |
| Author | Zahra Mojallal Tabatabaei | en |
| Author | Marjan Azimzadeh Arani | en |
| Author | Sogol Jafari-Ashtiani | en |
| Author | Mahsa Hashemian | en |
| Author | Parham Foroumadi | en |
| Author | Azadeh Yahya-Meymandi | en |
| Author | Setareh Moghimi | en |
| Author | Mohammad Hassan Moshafi | en |
| Author | Peiman Norouzi | en |
| Author | Susan Kabudanian Ardestani | en |
| Author | Alireza Foroumadi | en |
| Issued Date | 2019-10-31 | en |
| Abstract | 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 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). | en |
| DOI | https://doi.org/10.22037/ijpr.2019.14547.12476 | en |
| Keyword | Leishmaniasis | en |
| Keyword | Promastigote | en |
| Keyword | 1 | en |
| Keyword | 3 | en |
| Keyword | 4-thiadiazole | en |
| Keyword | MTT assay | en |
| Keyword | Synthesis | en |
| Publisher | Brieflands | en |
| Title | Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major | en |
| Type | Original Article | en |
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