A5030829054- Malaria Research and Control
- Computational Drug Discovery Methods
- Synthesis and biological activity
- HIV/AIDS drug development and treatment
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Analysis
- Synthesis of Organic Compounds
- Glycosylation and Glycoproteins Research
- Plant Pathogens and Fungal Diseases
- Traditional and Medicinal Uses of Annonaceae
- Metal complexes synthesis and properties
- Organometallic Complex Synthesis and Catalysis
- Magnetism in coordination complexes
- Drug-Induced Hepatotoxicity and Protection
- Ferrocene Chemistry and Applications
- Molecular Sensors and Ion Detection
- Receptor Mechanisms and Signaling
- vaccines and immunoinformatics approaches
- Mass Spectrometry Techniques and Applications
- Synthesis and Biological Evaluation
- Chemical Synthesis and Reactions
- Research on Leishmaniasis Studies
- Parasitic Diseases Research and Treatment
- Parasites and Host Interactions
- Synthesis and Biological Activity
GlaxoSmithKline (Spain)
2002-2018
GlaxoSmithKline (Netherlands)
2016
GlaxoSmithKline (United Kingdom)
2008-2011
Wellcome Trust
2008
Consejo Superior de Investigaciones Científicas
1997-2000
Hospital Universitario Severo Ochoa
2000
Wellcome Library
2000
Instituto de Química Orgánica General
1997
Instituto de Química Médica
1993-1997
Centre National de la Recherche Scientifique
1997
A series of diaryl ether substituted 4-pyridones have been identified as having potent antimalarial activity superior to that chloroquine against Plasmodium falciparum in vitro and murine yoelii vivo. These were derived from the anticoccidial drug clopidol through a systematic study effects varying side chain on activity. Relative most active compounds show >500-fold improvement IC50 for inhibition P. about 100-fold with respect ED50 mice. shown elsewhere act selectively by mitochondrial...
In 2010, GlaxoSmithKline published the structures of 13533 chemical starting points for antimalarial lead identification. By using an agglomerative structural clustering technique followed by computational filters such as activity, physicochemical properties, and dissimilarity to known structures, we have identified 47 optimization. Their are provided. We invite potential collaborators work with us discover new clinical candidates.
Malaria is still one of the most prevalent parasitic infections in world, with half world's population at risk for malaria. The effectiveness current antimalarial therapies, even that recent class drugs (artemisinin-combination ACTs), under continuous threat by spread resistant Plasmodium strains. As a consequence, there an urgent requirement new drugs. We previously reported identification 4(1H)-pyridones as novel series potent activities. low solubility was identified issue to address. In...
Antiparasitic oral drugs have been associated to lipophilic molecules due their intrinsic permeability. However, these kind of are numerous adverse effects, which extensively studied. Within the Tres Cantos Antimalarial Set (TCAMS) we identified two small, soluble and simple hits that even presenting antiplasmodial activities in range 0.4–0.5 μM able show vivo activity.
A convenient synthesis of the proton-ionizable crown 3 is reported that uses dibutyltin oxide. In acetonitrile, reaction (LH(2)) with phenethylamine and homoveratrylamine (molar ratio 1:2) affords solid dinuclear complexes [LH(2)]2RNH(2) (4a,b), which spectroscopic (FAB-MS, IR, (1)H (13)C NMR) data point toward a strong participation pyrazole nitrogens in amine complexation. DMSO-d(6) solution, NMR study demonstrates formation situ analogous neutral 4a-d[LH(2)]2RNH(2) or charged...
A new synthesis of the antimalarial clinical candidate GSK932121 is described. This approach has two key reactions, selective acylation an unprotected 3-hydroxymethyl-5-methyl isoxazole and reductive N-O bond cleavage previously functionalized derivative, to give 4-(1H)pyridone ring present in final structure. The complete consists 5 steps (versus 10 published reports) enabled preparation material kilogram scale support studies.
The Uniting to Combat Neglected Tropical Diseases partners, including the US, UK, UAE and other national governments, along with 13 pharmaceutical industry businesses, World Bank, Bill Melinda Gates Foundation, neglected tropical disease-endemic countries, announced that they are join together drive research innovation for treatment of diseases. collaboration will see countries work alongside these organizations goal fueling R&D treatments ten diseases in support WHO's 2020 goals. Isaac...
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
Abstract For see ChemInform in Full Text.