Structure–Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials
John A. Gilleran,
Kutub Ashraf,
Melvin Delvillar
et al.
Abstract:Controlling malaria requires new drugs against Plasmodium falciparum. The P. falciparum cGMP-dependent protein kinase (PfPKG) is a validated target whose inhibitors could block multiple steps of the parasite's life cycle. We defined the structure− activity relationship (SAR) of a pyrrole series for PfPKG inhibition. Key pharmacophores were modified to enable full exploration of chemical diversity and to gain knowledge about an ideal core scaffold. In vitro potency against recombinant PfPKG and human PKG were u… Show more
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