| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370930 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
A series of compounds containing 2-substituted imidazoles has been synthesized from imidazole and tested for its biological activity against human African trypanosomiasis (HAT). The 2-substituted 5-nitroimidazoles such as fexinidazole (7a) and 1-[4-(1-methyl-5-nitro-1H-imidazol-2-ylmethoxy)-pyridin-2-yl-piperazine (9e) exhibited potent activity against T. brucei in vitro with low cytotoxicity and good solubility. The presence of the NO2 group at the 5-position of the imidazole ring in 2-substituted imidazoles is the crucial factor to inhibit T. brucei.
Graphical abstractA series of compounds containing a 2-substituted imidazole ring has been synthesized from imidazole and tested for its biological activity against human African trypanosomiasis (HAT) along with its cytotoxicity and solubility.Figure optionsDownload full-size imageDownload as PowerPoint slide
