Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities (Publications)
plausible explanation for lack of significant activity of the inhibitors in the in vivo Pb mouse malaria model
The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to <em>Plasmodium falciparum</em> parasite resistance (Publications)
mode of action. This preclinical candidate may offer the potential for a single low-dose cure for malaria.
Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities (Publications)
plausible explanation for lack of significant activity of the inhibitors in the in vivo Pb mouse malaria model
Antimalarial benzoheterocyclic 4-aminoquinolines: structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies (Publications)
for antiplasmodial activity against K1 (multidrug resistant) and NF54 (sensitive) strains of the malaria parasite Plasmodium falciparum. Structure-activity relationship studies led to the identification
Conformational aspects in the design of inhibitors for serine hydroxymethyltransferase (SHMT): biphenyl, aryl sulfonamide, and aryl sulfone motifs (Publications)
Malaria remains a major threat to mankind due to the perpetual emergence of resistance against marketed drugs. Twenty-one pyrazolopyran-based inhibitors bearing terminal biphenyl, aryl sulfonamide, or
A <em>Plasmodium </em>membrane receptor platform integrates cues for egress and invasion in blood forms and activation of transmission stages (Publications)
Critical events in the life cycle of malaria-causing parasites depend on cyclic guanosine monophosphate homeostasis by guanylyl cyclases (GCs) and phosphodiesterases, including merozoite egress or invasion
Synthesis and in vitro and in vivo evaluation of antimalarial polyamines (Publications)
falciparum. In an effort to expand the structure-activity relationship of this compound class towards malaria, we have prepared and biologically tested a library that includes benzamide and 3-phenylpropanamide
Open source drug discovery: highly potent antimalarial compounds derived from the Tres Cantos arylpyrroles (Publications)
The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for
TKK130 is a 3-hydroxy-propanamidine (HPA) with potent antimalarial <em>in vivo</em> activity and a high barrier to resistance (Publications)
Malaria continues to pose a significant burden on populations in endemic areas and requires innovative treatment options. Here, we report the synthesis and preclinical evaluation of the novel 3-hydrox
Decreased in vitro susceptibility of <em>Plasmodium falciparum</em> isolates to artesunate, mefloquine, chloroquine, and quinine in Cambodia from 2001... (Publications)
from patients enrolled in therapeutic efficacy studies (TES) conducted by the Cambodian National Malaria Control Program for the routine efficacy monitoring of artemisinin-based combination therapy (ACT)