Abstract

More than half a century ago, scientists found penicillin and sulfonamide as the cure for treating bacterial infections. They have continued to put a significant effort into screening soil samples and natural products for the new classes of antibiotics. However, resistance to the corresponding antibiotics was quickly found after discovery of these antibiotics.1 One of the major antibiotic resistance mechanisms is the overproduction of β-lactamases. New Delhi Metallo-β-lactamase-1 (NDM-1) is considered the most worrisome β-lactamases due to its broad-spectrum effect on all clinically available β-lactam antibiotics, including the last resort antibiotics.2 Until now, no NDM-1 inhibitor has been approved on the market. Therefore, there is a need to develop effective NDM-1 inhibitors. Recently, we have designed several quinoline based NDM-1 inhibitors that showed good MIC results against NDM-1 producing E. coli when synergistically applied with meropenem. 

Reference:

1. Bush, K.; Page, M. G. P. J. Pharmacokinet. Pharmacodyn, 2017, 44 (2), 113 – 132.
2. Rogers, B. A.; Sidjabat, H. E.; Silvey, A.; Anderson, T. L.; Perera, S.; Li, J.; Paterson, D. L. Microb. Drug Resist. 2013, 19 (2), 100–103.