Anti-Infective Antibacterial Agents against Mycobacterium Tuberculosis and other Mycobacterium Species

Project ID: D2016-53

Background

Mycobacterium tuberculosis is an acid-fast gram-positive bacterium that causes tuberculosis (TB). TB ranks first for the number of deaths in humans caused by an infectious agent. It has been difficult to eradicate TB even though the infection is treatable. Treatment for TB takes at least 6 months and, sometimes, up to 2 years. Often, patients do not comply with the entire treatment regimen due to the high numbers of pills per day and the associated side effects. The discontinuation of treatment results in drug resistance. Therefore, there is an immediate need for drugs with improved efficacy and reduced toxicity.

Invention Disclosure
Researchers at he University of Toledo have developed new antimicrobial agents that are effective against human and veterinary pathogens, particularly acid-fast organisms such as Mycobacterium tuberculosis. The compounds show improved efficacy and activity well below toxicity to human monocytic cells.

Applications

• The compounds may be used for the treatment of drug-resistant tuberculosis
• The compounds may also be used for the treatment of other infections resulting from other Mycobacterium species

Advantages

• The compounds have unique composition and possess unique chemistry in preparation of derivatives
• The compounds developed exhibit good activity to toxicity ratio. The compounds may be active at concentrations 20-fold lower than toxicity
• The compounds have shown potency (MIC = 0.2 – 0.44 µM) against Mycobacterium tuberculosis strains resistant to Isoniazid, Rifampicin and fluoroquinolones. This suggests activity against multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains

IP Status:  10,604,752B2

Publication:                       Thanna S et al., Synthesis and evaluation of new 2-aminothiophenes against Mycobacterium tuberculosis. Organic & Biomolecular Chemistry, 2016, 14(25):6119-6133