Abstract
The need for the identification of novel antimicrobial agents is greater than
ever due to the emergence of multidrug resistance (MDR) among clinically important
pathogens which pose serious threats to public health worldwide. Unfortunately, the
pace of discovery and development of new antimicrobial agents to treat MDR infection
has significantly slowed down. Identifying new targets and chemical classes is not
easy, and reinvestigating old strategies by testing new compounds on known targets
and expecting novel outcomes, seems not only a failure but a border on insanity. The
development of new antimicrobial agents, chiefly those with novel mechanism(s) of
action, remains essential, but this alone does not guarantee success. It is important to
explore diverse information from multiple strategies, including multi-omics,
bioinformatics, system biology and other non-conventional approaches. In this chapter,
we give a brief background on the importance of antimicrobial drug discovery, detail
several discovery platforms from target-based discovery to the current innovative
strategy being evaluated, and list the challenges alongside each platform.