| Autor: |
Cheng, G., Muench, S.P., Zhou, Y., Afanador, G.A., Mui, E.J., Fomovska, A., Lai, B.S., Prigge, S.T., Woods, S., Roberts, C.W., Hickman, M.R., Lee, P.J., Leed, S.E., Auschwitz, J.M., Rice, D.W., McLeod, R. |
| Jazyk: |
angličtina |
| Rok vydání: |
2013 |
| ISSN: |
0960-894X |
| Popis: |
Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential enzyme for parasite survival. In view of triclosan’s poor druggability, which limits its therapeutic use, a new set of B-ring modified analogs were designed to optimize its physico-chemical properties. These derivatives were synthesized and evaluated by in vitro assay and TgENR enzyme assay. Some analogs display improved solubility, permeability and a comparable MIC50 value to that of triclosan. Modeling of these inhibitors revealed the same overall binding mode with the enzyme as triclosan, but the B-ring modifications have additional interactions with the strongly conserved Asn130. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect