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Discovery of Novel Pharmacophores Inhibiting the Growth of Mycobacterium tuberculosis

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

Market:
TB therapeutics

Inventors:
Robert C. Goldman (NIAID) et al.

Patent Status:
DHHS Reference No. E-310-2008/0 --
U.S. Provisional Application No. 61/092,710 filed 28 Aug 2008

Relevant Publication:

Manuscript in preparation

Licensing Status:

Available for exclusive or non-exclusive 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-Anti-Bacterial
Infectious Diseases -Therapeutics


For Additional Information Please Contact:
Kevin Chang Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/435-5018
Email: changke@mail.nih.gov
Fax: 301/402-0220

Web Ref: 1855

Last Updated On: 12/08


 
 
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