PDF catalyzes the formylation-deformylation process which is essential for bacterial protein synthesis, its growth and survival is the major difference between human and bacterial cell. PDF represents most promising bacterial target in the search of novel antibiotics that lack cross-resistance to existing drugs. A number of PDFIs have been introduced till date. Actinonin is the first known PDF inhibitor. Two PDFIs BB-83698 and VIC-104959 (LBM-415; NVP-PDF-713) have entered into clinic trials in humans.