Tuberculosis remains the leading cause of mortality worldwide. The facts relating to a front-line antitubercular drug isoniazide and its analogues. The antitubercular pharmacophore moiety of isoniazide has been introduced in various compounds to improve their antitubercular activity against mycobacterium, as well as their multidrug resistant mycobacterium strains. Various compounds like Schiff bases, hydrazones, hydrazides and metal complexes of isoniazid have shown good antitubercular activity. A series of isoniazid analogues have been evaluated for their activity against Mycobacterium tuberculosis. Some compounds exhibited significant antitubercular activity when compared with first line drugs like isoniazid and rifampicin and could be a good starting spot to develop new compounds in the fight against multi-drug resistant tuberculosis.