|
|||||
|
|
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG) |
|
| Authors: | Denise J Tsagris Kristian Birchall Nathalie Bouloc Jonathan M Large Andy Merritt Ela Smiljanic-Hurley Mary Wheldon Keith H Ansell Catherine Kettleborough David Whalley Lindsay B Stewart Paul W Bowyer David A Baker Simon A Osborne |
| Institution: | 1. LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK;2. Faculty of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK |
| Abstract: | A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria. |
| Keywords: | Plasmodium falciparum Malaria Thiazole |
| 本文献已被 ScienceDirect 等数据库收录！ | |