Discovery Projects - Grant ID: DP140103996

Funding Activity

Website
http://dataportal.arc.gov.au/NCGP/Web/Grant/Grant/DP140103996

Funding Status
Closed

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Funded Activity Summary

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.

Funded Activity Details

Start Date: 01-01-2014

End Date: 30-11-2017

Funding Scheme: Discovery Projects

Funding Amount: $420,000.00

Funder: Australian Research Council

Research Topics

ANZSRC Field of Research (FoR)

Medicinal and Biomolecular Chemistry | Cheminformatics and Quantitative Structure-Activity Relationships | Organic Chemical Synthesis | Biologically Active Molecules

ANZSRC Socio-Economic Objective (SEO)

Respiratory System and Diseases (incl. Asthma) | Expanding Knowledge in the Medical and Health Sciences | Infectious Diseases |

Other Keywords

Biologically Active Molecules | Cheminformatics and Quantitative Structure-Activity Relationships | Expanding Knowledge in the Medical and Health Sciences | Infectious Diseases | Medicinal and Biomolecular Chemistry | Organic Chemical Synthesis | Respiratory System and Diseases (incl. Asthma)

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