Graphical abstract Focussed studies on imidazopyridine inhibitors of Plasmodium falciparum cyclic GMP-dependent protein kinase ( Pf PKG) have significantly advanced the series towards desirable in vitro property space. LLE-based approaches towards combining improvements in cell potency, key physicochemical parameters and structural novelty are described, and a structure-based design hypothesis relating to substituent regiochemistry has directed efforts towards key examples with well-balanced potency, ADME and kinase selectivity profiles.
All Keywords
【저자키워드】 malaria, SAR, Plasmodium falciparum, cGMP, Protein kinase G, Imidazopyridine,
【저자키워드】 malaria, SAR, Plasmodium falciparum, cGMP, Protein kinase G, Imidazopyridine,