The ethos driving the antibiotic discovery program at Wockhardt has been to evolve projects that stand strong on the foundation of innovative chemistry driven MOA differentiation which leads to candidate drugs inheriting clinical features enabling fulfilment of challenging unmet needs. All the novel drug candidates have been designed to ensure clinical viability through broadly targeting clinically validated drug targets. The guiding principle for the discovery team has been to evolve antibiotics that are patient as well as clinician friendly, simple to use and offer a class-leading safety and efficacy outcome. Accordingly, discovery program at Wockhardt has focused on bacterial DNA gyrase/topoisomerae IV inhibitors (fluoroquinolones), protein synthesis inhibitors (oxazolidinones and macrolide/ketolide), β-lactam/β-lactamase inhibitor combinations and β-lactam/non-β-lactam, β-lactam enhancer combinations). Remarkably, from each class, the team’s insight led to identification of clinical candidates, with two of them gaining market approval and others progressing to the final Phase III stage of clinical development. The salient chemical features of Wockhardt’s NCEs are chiral molecules synthesized by putting together non-commercial synthons based on structure-activity-relationship (SAR)-driven inferences. These molecules were put through discriminating biological screens at an early stage, instead of the sequential battery of traditional tests.