Resistant pathogenic microbial strains are emerging at a rate that far exceeds the pace of new anti-infective
drug development. In order to combat resistance development, there is pressing need to develop novel class of antibiotics
having different mechanism of action in comparison to existing antibiotics. Antimicrobial peptides (AMPs) have been
identified as ubiquitous components of innate immune system and widely regarded as a potential source of future
antibiotics owing to a remarkable set of advantageous properties ranging from broad spectrum of activity to low
propensity of resistance development. However, AMPs present several drawbacks that strongly limit their clinical
applicability as ideal drug candidates such as; poor bioavailability, potential immunogenicity and high production cost.
Thus, to overcome the limitations of native peptides, peptidomimetic becomes an important and promising approach. The
different research groups worldwide engaged in antimicrobial drug discovery over the past decade have paid tremendous
effort to design peptidomimetics. This review will focus on recent approaches in design of antimicrobial peptidomimetics
their structure–activity relationship studies, mode of action, selectivity & toxicity.