Structural analysis has been successfully implemented recently to obtain valuable information on the mycobacterial cell wall components, many of which have formed the basis for biosynthesis and functional studies towards developing better drugs and possible vaccines. The highly complex and well organized structure unique to mycobacteria, represents the best target for novel antimycobacterial agents. Until recently, our knowledge of the enzymes responsible for the biogenesis of the cell wall components was almost negligible. The pathways are now being elucidated in several laboratories. Highlights of this review include significant advances in the structure and biochemistry of the major cell wall components and potential targets for generation of new drugs.