Discovery of Novel Pharmacophores Inhibiting the Growth of Mycobacterium tuberculosis
Posted Jun 13 2010 5:00pm
Description of Invention: Tuberculosis (TB) caused by Mycobacterium tuberculosis infects roughly one third of the world population and approximately 8 million people develop TB annually. The emergence of multi-drug resistant (MDR) and extensively drug-resistant (XDR) TB strains highlight the need for new drugs against TB. The inventions described herein are small molecules with drug-like properties that inhibit the growth of Mycobacterium tuberculosis. The compounds were discovered utilizing high-throughput screening of a 101,000 compound library. Three hundred active compounds inhibit Mycobacterium tuberculosis growth by 90% or greater in in vitro assays with MIC values ranging from 1.6 to less than 0.1 micrograms/ml, and showing minimal toxicity in tissue culture cells. Structure similarity analyses of the compounds reveal 44 chemical clusters representing 250 active compounds.
Applications: Treatment of TB infections
Advantages: Novel drug candidates against TB
Development Status: In vitro data can be provided upon request
Inventors: Robert C Goldman (NIAID)
Relevant Publication:
Manuscript in preparation
Licensing Status: Available for licensing.
Collaborative Research Opportunity: The NIAID, OTD, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize this "Discovery of Novel Pharmacophores Inhibiting the Growth of Mycobacterium Tuberculosis". Please contact Anna Amar at 301-451-3525 for more information.
Portfolios: Infectious Diseases Infectious Diseases - Therapeutics In-vitro Data
For Additional Information Please Contact: Kevin Chang Ph.D. NIH Office of Technology Transfer 6011 Executive Blvd. Suite 325, Rockville, MD 20852 United States Email: changke@mail.nih.gov Phone: 301-435-5018 Fax: 301-402-0220
Description of Invention:
Tuberculosis (TB) caused by Mycobacterium tuberculosis infects roughly one third of the world population and approximately 8 million people develop TB annually. The emergence of multi-drug resistant (MDR) and extensively drug-resistant (XDR) TB strains highlight the need for new drugs against TB. The inventions described herein are small molecules with drug-like properties that inhibit the growth of Mycobacterium tuberculosis. The compounds were discovered utilizing high-throughput screening of a 101,000 compound library. Three hundred active compounds inhibit Mycobacterium tuberculosis growth by 90% or greater in in vitro assays with MIC values ranging from 1.6 to less than 0.1 micrograms/ml, and showing minimal toxicity in tissue culture cells. Structure similarity analyses of the compounds reveal 44 chemical clusters representing 250 active compounds.
Applications:
Treatment of TB infections
Advantages:
Novel drug candidates against TB
Development Status:
In vitro data can be provided upon request
Inventors:
Robert C Goldman (NIAID)
Relevant Publication:
Licensing Status:
Available for licensing.
Collaborative Research Opportunity:
The NIAID, OTD, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize this "Discovery of Novel Pharmacophores Inhibiting the Growth of Mycobacterium Tuberculosis". Please contact Anna Amar at 301-451-3525 for more information.
Portfolios:
Infectious Diseases
Infectious Diseases - Therapeutics
In-vitro Data
For Additional Information Please Contact:
Kevin Chang Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: changke@mail.nih.gov
Phone: 301-435-5018
Fax: 301-402-0220
Ref No: 1862
Updated: 06/2010