| Autor: |
Akama, T., Zhang, Y. K., Freund, Y. R., Berry, P., Lee, J., Easom, E. E., Jacobs, R. T., Plattner, J. J., Witty, M. J., Peter, R., Rowan, T. G., Gillingwater, K., Brun, R., Nare, B., Mercer, L., Xu, M., Wang, J., Liang, H. |
| Rok vydání: |
2017 |
| Předmět: |
|
| DOI: |
10.5451/unibas-ep57728 |
| Popis: |
Novel l-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T. vivax) parasites. The study identified 4-fluorobenzyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbonyl)-l-valinate (5, AN11736), which showed IC50 values of 0.15 nM against T. congolense and 1.3 nM against T. vivax, and demonstrated 100% efficacy with a single dose of 10 mg/kg against both T. congolense and T. vivax in mouse models of infection (IP dosing) and in the target animal, cattle, dosed intramuscularly. AN11736 has been advanced to early development studies. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
