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
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
Analogues of thiolactomycin as potential antimalarial agents (Publications)
fatty acid synthase, were synthesized and evaluated for their ability to inhibit the growth of the malaria parasite Plasmodium falciparum. Alkylation of the C4 hydroxyl group led to the most significant increase
Epidemiology of multiple<em> Plasmodium falciparum </em>infections. 4. Age dependence of the multiplicy of <em>Plasmodium falciparum</em> infections... (Publications)
result, peak prevalence was reached in 3-5 years old children. However, the prevalence of clinical malaria (estimated from the excess risk of axillary temperatures > or = 37.5 degrees C attributable to p
Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2 (Publications)
for antiplasmodial activity against NF54 (sensitive) and K1 (multidrug resistant) strains of the malaria parasite Plasmodium falciparum and evaluated for both aqueous solubility and metabolic stability
Potent antimalarials with development potential identified by structure-guided computational optimization of a pyrrole-based dihydroorotate... (Publications)
DHODH inhibitors have great potential for use in prophylaxis, which represents an unmet need in the malaria drug discovery portfolio for endemic countries, particularly in areas of high transmission in Africa
Cytochrome P450-mediated metabolism and CYP Inhibition for the synthetic peroxide antimalarial OZ439 (Publications)
OZ439 is a potent synthetic ozonide evaluated for the treatment of uncomplicated malaria. The metabolite profile of OZ439 was characterized in vitro using human liver microsomes combined with LC/MS-MS
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.
Differential infectivity of Plasmodium for mosquitoes (Publications)
The four human malarias - Plasmodium falciparum, P. vivax, P. ovale and P. malariaecan - canonly be transmitted by mosquitoes of the genus Anopheles, although not all species (nor all strains) of these
Additional blood meals increase sporozoite infection in <em>Anopheles</em> mosquitoes but not <em>Plasmodium falciparum</em> genetic diversity (Publications)
multiple blood meals on the number of P. falciparum genotypes developing from polyclonal natural human malaria infections (field-isolates) remains unexplored. Here, we experimentally infect An. gambiae with P