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Diamidines as antitrypanosomal, antileishmanial and antimalarial agents.
  • K. Werbovetz
  • Medicine
  • Current opinion in investigational drugs
  • 1 February 2006
TLDR
The selectivity of diamidines against trypanosomes, Leishmania and Plasmodium is rationalized through mechanism-of-action studies and an overview of the antiprotozoal activities of newer diamidine and diamidine prodrugs is presented. Expand
Novel Arylimidamides for Treatment of Visceral Leishmaniasis
TLDR
It is demonstrated that arylimidamides are a promising class of molecules that possess good antileishmanial activity and desirable pharmacokinetics and should be considered for further preclinical development as an oral treatment for VL. Expand
Antileishmanial Activities of Several Classes of Aromatic Dications
TLDR
The structure-activity relationships demonstrate the potent antileishmanial activity of several aromatic dications and provide valuable information for the future design and synthesis of more potent antiparasitic agents. Expand
Isoflavonoids and other compounds from Psorothamnus arborescens with antiprotozoal activities.
TLDR
The studies suggest that the isoflavone skeleton deserves further investigation as a template for novel antileishmanial and trypanocidal compounds. Expand
Purification, characterization, and drug susceptibility of tubulin from Leishmania.
TLDR
Purified leishmanial tubulin is recognized by commercially available anti-tubulin antibodies and displays concentration dependent assembly in vitro, and electrophilic compounds such as phenyl arsenoxide and 4-chloro-3,5-dinitro-alpha, alpha,alpha,alpha-trifluorotoluene (chloralin), which are of interest as traditional and experimental antiparasitic agents, inhibit the assembly of leishmania tubulin in vitro as well. Expand
Cellular effects of leishmanial tubulin inhibitors on L. donovani.
TLDR
Tubulin is validated as a suitable antileishmanial drug target and the cellular effects of the mammalian antimicrotubule agents ansamitocin P3, taxol, and hemiasterlin on Leishmania donovani promastigotes provide criteria to assess the cellular mechanism of action of new candidate antileishesmanial agents. Expand
α-Tubulin Mutations Alter Oryzalin Affinity and Microtubule Assembly Properties To Confer Dinitroaniline Resistance
TLDR
These data provide additional support for the proposed dinitroaniline binding site on α-tubulin and validate the use of T. thermophila for expression of genetically homogeneous populations of mutant tubulins for biochemical characterization. Expand
Novel amidines and analogues as promising agents against intracellular parasites: a systematic review
TLDR
This review summarizes the knowledge on amidines and analogues with respect to their synthesis, pharmacological profile, mechanistic and biological effects upon a range of intracellular protozoan parasites to contribute to the future design and structure optimization of new aromatic dicationic compounds as novel antiparasitic drug candidates. Expand
Natural products from plants as drug candidates and lead compounds against leishmaniasis and trypanosomiasis.
TLDR
The antikinetoplastid activities of plant-derived natural products reported in the literature are outlined and an overview of mechanistic studies that have been conducted with these compounds are provided. Expand
Antiprotozoal compounds from Psorothamnus polydenius.
TLDR
Bioactivity-guided fractionation of the methanolic extract of Psorothamnus polydenius yielded the new chalcone 2,2',4'-trihydroxy-6'-methoxy-3',5'-dimethylchalcone (2), together with six other known compounds, which were tested in vitro for their antiprotozoal activity against Leishmania donovani and Trypanosoma brucei. Expand
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