A5053604740- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Malaria Research and Control
- Parasites and Host Interactions
- Bioactive Compounds and Antitumor Agents
- Traditional and Medicinal Uses of Annonaceae
- Computational Drug Discovery Methods
- Insect and Pesticide Research
- Synthesis and biological activity
- Toxin Mechanisms and Immunotoxins
- Biochemical and Molecular Research
- X-ray Diffraction in Crystallography
- HIV/AIDS drug development and treatment
- Crystallization and Solubility Studies
- Insect Pest Control Strategies
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Catalytic Reactions
- Phytochemical compounds biological activities
- Cancer therapeutics and mechanisms
- Mosquito-borne diseases and control
- Eosinophilic Disorders and Syndromes
- Synthesis and bioactivity of alkaloids
- Drug Transport and Resistance Mechanisms
- Parasitic Infections and Diagnostics
London School of Hygiene & Tropical Medicine
2015-2025
University of London
2011-2021
The University of Tokyo
2019
University of York
2014-2019
Jawaharlal Institute of Post Graduate Medical Education and Research
2019
University of Pennsylvania
2019
Fundação Oswaldo Cruz
2019
Cooch Behar Panchanan Barma University
2018
Liverpool School of Tropical Medicine
2015
Drugs for Neglected Diseases Initiative
2005-2015
We have investigated the effects in vitro of a series bisphosphonates on proliferation Trypanosoma cruzi, brucei rhodesiense, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum. The results show that nitrogen-containing type used bone resorption therapy significant activity against parasites, with aromatic species having some cases nanomolar or low-micromolar IC50 values parasite replication (e.g. o-risedronate, = 220 nM for T. rhodesiense; risedronate, 490 gondii). In...
Trypanothione reductase (TR) is both a valid and an attractive target for the design of new trypanocidal drugs. Starting from menadione, plumbagin, juglone, three distinct series 1,4-naphthoquinones (NQ) were synthesized as potential inhibitors TR Trypanosoma cruzi (TcTR). The parent molecules functionalized at carbons 2 and/or 3 by various polyamine chains. Optimization TcTR inhibition specificity versus human disulfide reductases was achieved with...
Artemisinin—the next generation: Efficacies of artemisone against the malaria parasite are substantially greater than those current artemisinin "gold standard", artesunate. Also, in contrast to most artemisinins it displays low lipophilicity and negligible neuro- cytotoxicity vitro vivo assays. Thus, drug offers promise for use artemisinin-based combination therapy. Supporting information this article is available on WWW under http://www.wiley-vch.de/contents/jc_2002/2006/z503071_s.pdf or...
The interaction of miltefosine with amphotericin B, sodium stibogluconate, paromomycin, and sitamaquine was assessed in vitro additionally for the first three combinations vivo. In interactions were indifferent combined B (mean sums fractional inhibitory concentrations [mean summation operatorFICs] ranging from 1.22 to 1.51 at 50% effective concentration [EC50] level 1.08 1.38 EC90 level), operatorFICs 1.33 1.0 1.02, respectively), paromomycin 0.79 0.93 EC50 0.77 1.35 level). Some synergy...
A method has been defined for infecting primary mouse peritoneal macrophages with amastigotes of Leishmania donovani in vitro, and analysing the response infected to treatment drugs. The growth intracellular was inhibited by all clinically used antileishmanial Toxic effects on were observed some Other experimental compounds active this system. This test is proposed as an initial screening discovery novel compounds.
The in-vitro activities of four anticancer alkyllysophospholipids, ET-18-OCH3 (edelfosine), hexadecylphosphocholine (miltefosine), ilmofosine and SRI 62-834, were determined with ED50 values for Leishmania donovani Trypanosoma cruzi amastigotes between 0.2 5.0 microM brucei trypomastigotes 7.0 50.8 microM. In BALB/c mice miltefosine the most active compounds 2.9 14.5 mg/kg x 5 doses against L. a suppressive effect on T. infections at 30 doses.
To combat drug resistance, new chemical entities are urgently required for use in next generation anti-malarial combinations. We report here the results of a medicinal chemistry programme focused on an imidazopyridine series targeting Plasmodium falciparum cyclic GMP-dependent protein kinase (PfPKG). The most potent compound (ML10) has IC