Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis

✍ Scribed by Bhupesh S. Samant; Mugdha G. Sukhthankar

• Book ID: 104005221
• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 294 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.12.040

✦ Synopsis

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-2yl-piperazine (9e) exhibited potent activity against T. brucei in vitro with low cytotoxicity and good solubility. The presence of the NO 2 group at the 5-position of the imidazole ring in 2-substituted imidazoles is the crucial factor to inhibit T. brucei.