| 摘要 |
Substituted pyridinylimidazoles SB203580 and SB202190 strongly inhibit replication and cause stage conversion from active tachyzoites to relatively dormant bradyzoites of the medically important, obligate intracellular parasite Toxoplasma gondii. The pyridinylimidazoles probably mediate these effects by acting on a presently unidentified homologue(s) of human p38-mitogen activated protein kinase present in the tachyzoites. SB203580 also significantly enhanced in vitro inhibition of T. gondii replication by the approved anti-toxoplasma drug pyrimethamine. The pyridinylimidazoles and related compounds disclosed herein could thus be significant adjuncts to currently available therapies. |
