Jain, V: Pyrazoline Derivatives as Antitubercular Agents

Mycobacterium tuberculosis (MTB), the pathogenic agent of tuberculosis (TB), is responsible for the death of 2 3 million people annually and for a global economic toll of $12 billion each year. Thus, there is an urgent need to develop new therapeutics for tuberculosis, to reduce the duration of treatment and to provide a more effective therapy for MDR TB and for latent tuberculosis infection. In the present investigation, a series of 4-(4-(dimethylamino) benzyl)-3-methyl-1H-pyrazol-5(4H)-one analogues of pyrazole were synthesized by cyclization of mannich base with hydrazine hydrate. The nitrogen functionality of 4-(4-(dimethylamino) benzyl)-3-methyl-1H-pyrazol-5(4H)-one was alkylated with different halogenated alkylated substituted chain in the presence of base. The chemical structure of compounds were proved by IR, MASS, 1HNMR spectroscopy data and elemental analysis. . The antitubercular activity of these compounds were evaluated by microdilution method against M. Tuberculosis H37Rv micobactrium strain of M. Tuberculosis compared with standard INH, RIF & ETM.