Tuberculosis is a highly contagious infectious disease triggered by Mycobacterium tuberculosis, which is widely spread by aerosol. The major site of infection is usually the lungs however the disease can attack any extra-pulmonary site as well, which is further diagnosis by necrotizing granulomatous inflammation. World Health Organization reported almost 8.9–10 million people are suffering from tuberculosis in 2019, including 56% men and 32% women, and 12% children. Multidrug-resistant tuberculosis (MDR-TB) is a medical condition in which Mycobacterium tuberculosis strains resistant to at least isoniazid and rifampicin. In-vitro studies suggest that several bioactive compounds and their synthetic derivatives obtained from plants, fungi, and marine organism possesses antimycobacterial affinity. Phenolic compounds such as dihydrocubebin, hinokinin, ethoxycubebin possess the antimycobacterial activity. Mycobacterial cell envelope antagonists have been shown to obstruct the synthesis of mycolic acids, arabinogalactan, and peptidoglycan, essential components of the mycobacterial cell wall. The paramount antituberculous drugs hamper the development of mycolic acids or the aid mechanism which links them to the cell membrane. Medicines targeting RNA synthesis encompass those that restrict the assembly of bacterial DNA-dependent RNA polymerases, that are indispensable enzymes for RNA synthesis. Various molecular pathways for the target to cure tuberculosis entail the targets of M. tuberculosis cell wall synthesis, energy metabolism, folate metabolism, DNA replication, and RNA synthesis. Interestingly, in preserving the health of patients diagnosed with tuberculosis, medicinal plants have tremendous advantages with limited side effects as compare to the standard drugs.