|
|||||
|
|
Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis |
|
| Authors: | Samant Bhupesh S Sukhthankar Mugdha G |
| Institution: | a Natural Product and Medicinal Chemistry (NPMC) research group, Division of Pharmaceutical chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa b Laboratory of Environmental Carcinogenesis, Department of Pathobiology, College of Veterinary Medicine, The University of Tennessee, Knoxville, TN 37996, USA |
| Abstract: | 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. |
| Keywords: | Fexinidazole Sleeping sickness African trypanosomiasis 2-Substituted 5-nitroimidazole |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |