Despite major antimicrobial therapeutic advancements, widespread use and misuse of antimicrobial drugs have increased antimicrobial drug resistance, posing a severe danger to public health. In particular, the emergence of multidrug-resistant bacteria has provided considerable difficulty in the treatment of pathogenic infections. As a result, the creation of novel drugs to treat resistant bacteria is one of the most significant disciplines of antimicrobial research today. TB therapy has recently gained a lot of attention, in addition to developing novel and efficient antibacterial drugs to battle multidrug-resistant illnesses. The use of a different class of drugs, such as well-known drugs, their derivatives, and various new heterocyclic compounds like nitroimidazoles, imidazole analogues, triazoles, imidazopyridines, quinolines, purines, as well as thioactomycin, mefloquine, deazapteridines, benzothiadiazine and other molecules such as benzoxazines, diterpenoids, tryptanthin and phenazine and toluidine analogues followed by many other classes of compounds and their effects are also discussed. As a result, current and newly found antitubercular drugs and their toxicities and mode of action have been focused.