Design and synthesis of novel monocyclic beta-lactam as antimycobacterial agents

The rebirth of tuberculosis and outbursts of multiple-drug-resistant (MDR) strains of Mycobacterium tuberculosis (TB) are reminders that new potent drugs are necessary. Due to overuse and misuse, the old repertories of TB drugs are not effective against most antimycobacterial strains. beta-lactam based drugs have served the humanity for more than seventy years in its war against bacterial infections and are responsible for saving millions of lives. However, they were not considered to have any antimycobacterial activity and, therefore, were completely ignored in the development of new antimycobacterial agents. Recent literature shows that beta-lactams do have antimycobacterial activity. The mapping of the genome of Mycobacterium tuberculosis will lead the way in the development of new effective antimycobacterials and to the creation of large libraries of compounds synthesized by combinatorial chemistry, which include the beta-lactam framework. We propose to design and synthesize novel monocyclic beta-lactam as antimycobacterial agents.