Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase (Publications)
Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were evaluated. Some of our compounds inhibited [...] inhibited TR, showed selectivity for TR over human glutathione reductase, and inhibited parasite growth in vitro. We propose that the quinazoline framework is a privileged structure that can be purposely modified
SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents (Publications)
is, Chagas disease and leishmaniasis. Azasterols, have been shown to have activity against the parasites which cause these diseases. In this paper we report synthesis of new azasterols and subsequent analysis [...] allowed us to derive preliminary pharmacophore models for the activity of the azasterols against the parasites which cause these diseases
Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase (Publications)
Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were evaluated. Some of our compounds inhibited [...] inhibited TR, showed selectivity for TR over human glutathione reductase, and inhibited parasite growth in vitro. We propose that the quinazoline framework is a privileged structure that can be purposely modified
SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents (Publications)
is, Chagas disease and leishmaniasis. Azasterols, have been shown to have activity against the parasites which cause these diseases. In this paper we report synthesis of new azasterols and subsequent analysis [...] allowed us to derive preliminary pharmacophore models for the activity of the azasterols against the parasites which cause these diseases
Parasiten als Ursache von Urtikaria: Helminthen und Protozooen als Auslöser der Nesselsucht? (Publications)
aware that parasitic diseases are increasingly common even in industrialized countries due to a steep rise in migration and international travel. This review presents the most important parasitic causes of
Parasiten als Ursache von Urtikaria: Helminthen und Protozooen als Auslöser der Nesselsucht? (Publications)
aware that parasitic diseases are increasingly common even in industrialized countries due to a steep rise in migration and international travel. This review presents the most important parasitic causes of
Caught in action: mechanistic insights into antibody-mediated inhibition of <em>Plasmodium merozoite</em> invasion (Publications)
Apical membrane antigen 1 (AMA1) plays an essential role in host cell invasion by apicomplexan parasites. A recent study by Collins et al. investigated the mode of action of an anti-AMA1 invasion-inhibitory [...] on a single conserved tyrosine residue in AMA1. Their findings reveal important new insights into parasite biology and are highly relevant for rational vaccine design
Caught in action: mechanistic insights into antibody-mediated inhibition of <em>Plasmodium merozoite</em> invasion (Publications)
Apical membrane antigen 1 (AMA1) plays an essential role in host cell invasion by apicomplexan parasites. A recent study by Collins et al. investigated the mode of action of an anti-AMA1 invasion-inhibitory [...] on a single conserved tyrosine residue in AMA1. Their findings reveal important new insights into parasite biology and are highly relevant for rational vaccine design
<em>In vitro</em> assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of <em>Plasmodium falciparum</em> (Publications)
to OZ277 were monitored by incorporation of [(3)H]hypoxanthine into parasite nucleic acids and by light-microscopic analysis of parasite morphology. Partitioning studies were performed with radiolabelled [...] OBJECTIVES: Using synchronous cultures of Plasmodium falciparum malaria, the stage sensitivity of the parasite to OZ277 (RBx-11160), the first fully synthetic antimalarial peroxide that has entered Phase II
A new approach to chemotherapy: drug-induced differentiation kills African trypanosomes (Publications)
replaces the VSG coat by procyclins; these proteins do not protect the parasite from lysis by serum components. Our study exploits the parasite-specific process of differentiation from bloodstream to procyclic [...] asis (sleeping sickness) is a neglected tropical disease caused by Trypanosoma brucei spp. The parasites are transmitted by tsetse flies and adapt to their different hosts and environments by undergoing
