DESIGN, SYNTHESIS AND EVALUATION OF ANTI TUBERCULAR ACTIVITY OF NOVEL TRIAZOLE DERIVATIVES

Substituted triazoles have received considerable attention during the last two decades as they are endowed with a variety of biological activities and have a wide range of therapeutic properties. The present work is concerned with the synthesis of fused 1, 2, 4-triazole derivatives with the objective of discovering novel and potent antitubercular agents that might be devoid of harmful side effects. 1-[amino (isonicotinoyl) carbonohydrazonoyl] guanidine (I) was prepared from isoniazide and cyanoguanidine and was cyclized to 2-(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl) guanidine (II) which was further converted into amino triazolo triazine derivatives (IIIa-g) by refluxing with the appropriately substituted benzaldehydes. The final compounds 10-substituted-2-(pyridin-4-yl)-6,10-dihydro-5H-pyrimido[2,d] [1,2,4] triazolo[1,5-a] [1,3,5] triazine-6-carboxylic acid (IVa-g) were obtained by refluxing different amino triazolo triazine derivatives (IIIa-g) with formaldehyde and sodium pyruvate in presence of HCl in methanolic medium. The newly synthesized compounds were screened for their antitubercular activity using a microplate alamar blue assay method and characterized on the basis of IR, (HNMR)-H-1 and Mass spectral studies.