DESIGN, SYNTHESIS AND EVALUATION OF ANTI TUBERCULAR ACTIVITY OF NOVEL TRIAZOLE DERIVATIVESAbstract
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 anti-tubercular 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, 1HNMR and Mass spectral studies.
N. R. Babu *, U. Kulandaivelu, G. S. N. K. Rao, R. R. Alavala, Y. Padmavathi and B. M. Reddy
Department of Pharmaceutical Chemistry, K. L. College of Pharmacy, K. L. Deemed to be University, Vaddeswaram, Guntur, Andhra Pradesh, India.
18 July 2019
01 November 2019
10 February 2020
01 June 2020