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
Strategies for conducting <em>Anopheles stephensi </em>surveys in non-endemic areas (Publications)
Anopheles stephensi, a malaria vector species previously only known from Asia, was first detected in Africa in Djibouti in 2012, has been subsequently collected in Ethiopia, Sudan, and Somalia, and may
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
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
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.
Assessment of the humoral and cell-mediated immunity against the <em>Plasmodium falciparum</em> vaccine candidates circumsporozoite protein and SPf66... (Publications)
responders, respectively. Anti-CS protein antibodies increased with age but showed no association to malaria indices or morbidity. No protective value was observed with T cell responses or with humoral response
Identification of a new chemical class of antimalarials (Publications)
The increasing spread of drug-resistant malaria strains underscores the need for new antimalarial agents with novel modes of action (MOAs). Here, we describe a compound representative of a new class of
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
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