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Antitrypanosomal and Antileishmanial Activities of Flavonoids and Their Analogues: In Vitro, In Vivo, Structure-Activity Relationship, and Quantitative Structure-Activity Relationship Studies
- D. Taşdemir, M. Kaiser, P. Rüedi
- Chemistry, BiologyAntimicrobial Agents and Chemotherapy
- 1 April 2006
A large set of flavonoid aglycones and glycosides were surveyed, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, T. cruzi, and Leishmania donovani, and generally, the test compounds lacked cytotoxicity in vitro and in vivo.
Experimental evolution of aging, growth, and reproduction in fruitflies.
- S. Stearns, M. Ackermann, M. Doebeli, M. Kaiser
- BiologyProceedings of the National Academy of Sciences…
- 28 March 2000
These results confirm the key role of extrinsic mortality rates in the evolution of growth, maturation, reproduction, and aging, and they do so with a selection regime that maintained selection on fertility throughout life while holding population densities constant.
Fexinidazole – A New Oral Nitroimidazole Drug Candidate Entering Clinical Development for the Treatment of Sleeping Sickness
- E. Torreele, Bernadette Bourdin Trunz, B. Pécoul
- Biology, MedicinePLoS Neglected Tropical Diseases
- 1 December 2010
Fexinidazole is shown to be a short-course, safe and effective oral treatment curing both acute and chronic HAT and that could be implemented at the primary health care level and the results of the preclinical pharmacological and safety studies indicate that fexinidrazole is a safe andeffective oral drug candidate with no untoward effects that would preclude evaluation in man.
SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis
The biological and pharmacokinetic properties of SCYX-7158 suggest that this compound will be efficacious and safe to treat stage 2 HAT, and is selected to enter preclinical studies, with expected progression to phase 1 clinical trials in 2011.
The differential genetic and environmental canalization of fitness components in Drosophila melanogaster
Measurements of environmental canalization for Drosophila melanogaster suggest that developmental mechanisms buffer the phenotype against both genetic and environmental disturbance, and suggest, less strongly, that inbreeding weakens canalization.
Bromopyrrole Alkaloids as Lead Compounds against Protozoan Parasites
Results indicate longamide B and dibromopalau’amine (11) to be promising trypanocidal and antileishmanial agents, while dispacamide B (3) and spongiacidin B (6) emerge as antimalarial lead compounds.
In vitro screening of traditional South African malaria remedies against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum.
Three hundred extracts were prepared from plants traditionally used in South Africa to treat malaria and screened in vitro for activity against Trypanosoma brucei rhodesiense, TryPanosoma cruzi, Leishmania donovani, and Plasmodium falciparum, finding notable results against all four protozoal parasites.
In vitro antiplasmodial screening of ethnopharmacologically selected South African plant species used for the treatment of malaria.
Inhibitory Activity of Marine Sponge-Derived Natural Products against Parasitic Protozoa
This is the first report of antiprotozoal activity of marine metabolites 1–14, and points out the potential of marine sponges in discovery of new antipro tozoal lead compounds.
Antiprotozoal steroidal saponins from the marine sponge Pandaros acanthifolium.
- E. Regalado, D. Taşdemir, M. Kaiser, N. Cachet, P. Amade, O. Thomas
- ChemistryJournal of Natural Products
- 8 July 2010
The chemical composition of the Caribbean sponge Pandaros acanthifolium was reinvestigated and led to the isolation of 12 new steroidal glycosides, namely, pandarosides E-J and their methyl esters (7-12), which showed in vitro activity against three or four parasitic protozoa.