Rapid method development in pharmaceutical analysis using quality-by-design principles. Chemical analysis using separation methods underpins all stages of drug design and analysis. This project will generate new approaches to greatly reduce the time taken to develop a new method of analysis. This will be achieved through development of new computerised techniques for rapid screening, selection and optimisation of analytical methods.
Fragment based screening to deliver drugs targeting tuberculosis and the gametocyte and liver stages of Plasmodium. This project will identify natural products that bind to critical proteins in malaria and tuberculosis to discover new ways to treat these diseases.
Linkage Infrastructure, Equipment And Facilities - Grant ID: LE120100071
Funder
Australian Research Council
Funding Amount
$290,000.00
Summary
Chemi–biology computational platform for lead discovery in infectious disease. A challenge in fighting infectious disease is in finding new bioactive compounds. This facility will provide a high performance computational environment designed to accelerate the discovery of quality compounds for use in anti-infective medicine.
Interrogating diarylquinoline toxicity with targeted organic synthesis. Bedaquiline is the only new first-line treatment with a new mechanism of action to treat TB in the last 40 years, approved by the FDA on 31 December 2012. Alarmingly, this compound, has significant toxicities. The hypothesis tested in this project is that decreasing lipophilicity and basicity in this class of compounds while retaining target affinity will decrease toxicity but retain anti-TB activity. The project aims to: sy ....Interrogating diarylquinoline toxicity with targeted organic synthesis. Bedaquiline is the only new first-line treatment with a new mechanism of action to treat TB in the last 40 years, approved by the FDA on 31 December 2012. Alarmingly, this compound, has significant toxicities. The hypothesis tested in this project is that decreasing lipophilicity and basicity in this class of compounds while retaining target affinity will decrease toxicity but retain anti-TB activity. The project aims to: synthesise novel heteroarylalkylamines distinct from bedaquiline and designed to be more polar, less basic, and metabolically more stable; and, test all successfully synthesised target compounds for mechanism-based anti-tuberculosis activity, hERG-mediated cardiotoxicity, metabolic instability, and phospholipidosis.Read moreRead less
BioPPSy: An open source BIOchemical Property Prediction SYstem. Computer software will be developed for the prediction of the pharmacokinetic properties of small molecules to assist in the development of new compounds with drug-like properties. The software will be made freely available to promote its use and further development.
Towards The Rational Design Of Calcium Sensing Receptor Allosteric Modulators For The Treatment Of Osteoporosis And Calcium Handling Disorders
Funder
National Health and Medical Research Council
Funding Amount
$741,390.00
Summary
Drugs that target the human calcium sensing receptor can be too strong or too weak, resulting in side effects or lack of efficacy. This proposal thus seeks to establish whether the strength of drug activity can be rationally altered and exploited to treat different disease states by fine-tuning CaSR activity in a disease-specific manner.
Bismuth Compounds And Materials As Antibacterial Agents
Funder
National Health and Medical Research Council
Funding Amount
$476,535.00
Summary
Antimicrobial resistance has been identified by the World Health Organisation as one of the greatest threats we face globally. The amount of effective antibacterial agents is rapidly diminishing. The threat of antimicrobial resistance is greatest in hospitals and health-care facilities. Our project aims to produce a new range of bismuth based antibacterial materials, which will be used in devices, coatings and surfaces in the clinic, to combat the rise of infections caused by resistant bacteria.
Development Of Peptide-based Scaffolds For Intracellular Cancer Targets
Funder
National Health and Medical Research Council
Funding Amount
$1,479,836.00
Summary
The overall aim of this project is to develop peptide-based drugs that are able to cross cell membranes and inhibit specific targets inside cells leading to more effective, safer and cost effective drugs for cancer. One potential outcome of the project will be new drug leads to treat melanoma and leukemia that are likely to be less toxic, more potent and less likely to develop resistance than current treatments.
Structure-based Design Of Inhibitors Of PimA - A New Target For Tuberculosis Therapy
Funder
National Health and Medical Research Council
Funding Amount
$666,246.00
Summary
Tuberculosis (TB) is a devastating disease that kills 2 million people worldwide each year and affects one-third of the entire human population. Bacterial resistance to existing antibiotics is an ever increasing problem, highlighting the need to develop new anti-TB drugs. The aim of this project is to develop specific inhibitors to target a protein that is essential for the survival of the tuberculosis bacterium.