Tuberculosis (TB) is one the most prevalent endemic lung infection caused by the pathogen Mycobacterium tuberculosis (Mtb). In spite of the availability of various combinations of antitubercular drugs with a six-month treatment regimen, the global TB situation is worsened by increased morbidity and mortality. Further, the control of TB has been exacerbated by the emergence of multidrug resistant, extremely drug resistant TB strains, and latent infection. TB drugs currently in use were discovered much before in the seventies and studies indicate that TB drug research remained silent for more than 40 years. To counteract this crisis, there is an urgent need to develop novel alternative antitubercular agents which can target processes that are critical for the growth and survival of the bacterium. Development of antitubercular agents via molecular hybridization strategies can therefore be imagined as a future toward a new dawn where the classical/conventional molecules usage will diminish and molecular hybrids emerge to bring over a dramatic improvement in the mechanism of action against Mycobacterium tuberculosis (Mtb). We herein review strategies for antitubercular drug discovery with an emphasis on molecular hybridization and provide examples of hybrid molecules as highly potential antitubercular agents for clinical use.