A5026691220- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Research on Leishmaniasis Studies
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Asymmetric Synthesis and Catalysis
- Catalytic Alkyne Reactions
- Traditional and Medicinal Uses of Annonaceae
- Cyclopropane Reaction Mechanisms
- Catalytic Cross-Coupling Reactions
- Synthetic Organic Chemistry Methods
- Oxidative Organic Chemistry Reactions
- Marine Sponges and Natural Products
- Catalytic C–H Functionalization Methods
- Crystallography and molecular interactions
- Microbial Natural Products and Biosynthesis
- Coenzyme Q10 studies and effects
- Malaria Research and Control
- Synthesis of Organic Compounds
- Synthesis and biological activity
- Synthesis and Reactivity of Heterocycles
- Plant-based Medicinal Research
- Chemical synthesis and alkaloids
- Synthesis and Biological Activity
- Click Chemistry and Applications
Monash University
2012-2014
Murdoch University
2012-2013
The University of Melbourne
2012
Bionomics (Australia)
2008-2011
Australian National University
2001-2003
A structure-activity relationship (SAR) guided design of novel tubulin polymerization inhibitors has resulted in a series benzo[b]furans with exceptional potency toward cancer cells and activated endothelial cells. The early lead compounds been substantially improved through the synergistic effect introducing conformational bias additional hydrogen bond donor to pharmacophore. Screening focused library potent for selectivity against over quiescent afforded...
Chagas disease, caused by the eukaryotic (protozoan) parasite Trypanosoma cruzi, is an alarming emerging global health problem with no clinical drugs available to treat chronic stage. Azole inhibitors of sterol 14α-demethylase (CYP51) were proven effective against Chagas, and antifungal posaconazole ravuconazole have entered trials in Spain, Bolivia, Argentina. Here we present x-ray structures T. cruzi CYP51 complexes two alternative drug candidates, pyridine derivatives...
We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor Trypanosoma cruzi (T. cruzi), causative agent Chagas disease, and results structure–activity investigations leading to potent analogues with low nM IC50s in a T. whole cell vitro assay. Lead compounds suppressed blood parasitemia virtually undetectable levels after once daily oral dosing mouse models infection. Compounds are chemically tractable, allowing rapid optimization target biological activity drug...
Oxazolidinones are powerful promoters of the Nazarov reaction, enabling cyclization conventionally resistant substrates to be achieved under mild conditions. They exert excellent regio- and torquoselective control in both conventional reaction giving cyclopentenones "interrupted" more highly substituted multistereocenter containing products.
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), is an increasing threat to global health. Available medicines were introduced over 40 years ago, have undesirable side effects, and give equivocal results of cure in chronic stage disease. We report development two compounds, 6 (S)-7, with PCR-confirmed curative activity a mouse model established T. infection after once daily oral dosing for 20 days at mg/kg 10 (S)-7. Compounds (S)-7 potent vitro activity, are...
A convenient method for the synthesis of 2-bromo-3-aroyl-benzo[b]furans from readily accessible precursors has been developed. The 2-bromo group employed as a versatile synthetic handle in both palladium-mediated couplings and direct nucleophilic substitutions to give access wide range 2-substituted-3-aroyl-benzo[b]furans.
A single step access to multiply substituted benzo[b]furans and indoles has been developed.
Background: Inhibitors of Trypanosoma cruzi with novel mechanisms action are urgently required to diversify the current clinical and preclinical pipelines. Increasing number diversity hits available for assessment at beginning discovery process will help achieve this aim. Results: We report evaluation multiple generated from a high-throughput screen identify inhibitors T. these studies two series currently in lead optimization. Lead compounds potently selectively inhibit growth vitro most...
The complex tetracyclic carbon skeleton of colombiasin A is conveniently accessed through an enantioselective intermolecular Diels–Alder–sulfoxide elimination–intramolecular Diels–Alder (DA–E–IMDA) sequence.
Reductive coupling of α,β-unsaturated acid chlorides A with alkynoyls B provides convergent access to Nazarov cyclization precursors, α-carboxy divinyl ketones C. Cyclization C gives an intermediate oxyallyl cation D, which can be trapped tethered arenes (Ar). The resultant products further cyclized through nucleophilic displacement suitable leaving groups X by OH give lactones (in a subsequent step). Where is chiral auxiliary (e.g., oxazolidinone) this strategy affords homochiral cyclopentanoids.
Abstract Human African Trypanosomiasis (HAT) is a disease caused by the parasite Trypanosoma brucei and classified as neglected tropical of concern in sub‐Saharan Africa. A scoping study has been undertaken to develop preliminary structure activity relationship tetrahydroisoquinoline scaffold. Fourteen compounds based around this core scaffold were synthesised evaluated for their against rhodesiense vitro . Initial results are promising with number analogues showing low micromolar inhibition...
Condensation of phenylephrine with different aldehydes, under Pictet-Spengler cyclisation conditions, afforded a series tetrahydroisoquinoline derivatives as mixtures cis/trans isomers. Single crystal X-ray analysis the dibenzoate derivative one 4-nitrophenyl isomers confirmed it to be trans isomer. The conformation cis isomer was determined through computational experiments and comparison predicted observed 1H NMR spectra, particularly magnitude coupling constants. Fourteen were then...
Abstract In the presence of an excess MesOH or TfOH, divinyl and aryl vinyl ketones bearing oxazolidinone auxiliary undergo efficient highly stereoselective cyclization to optically active cyclopentenone derivatives.
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