Antibiotic resistance is an alarming multifaceted problem, and it is predicted to be one of the greatest threats to human health in the next few decades. Once antibiotic resistance is allowed to continue uncontrollably, we may enter a ‘post-antibiotic era’ of medicine, in which even a minor infection may become lethal. In the light of this global problem, we aimed to tackle ABR through three approaches including building multivalent glycomimetics, developing chimeric antibiotics, and modifying mutilin-type antibiotics.