DESIGN, SYNTHESIS AND EVALUATION OF ANTI TUBERCULAR ACTIVITY OF NOVEL TRIAZOLE DERIVATIVES
AbstractSubstituted 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.
Article Information
46
2920-2925
556
878
English
IJPSR
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.
nayakaraghavendrababu@gmail.com
18 July 2019
01 November 2019
10 February 2020
10.13040/IJPSR.0975-8232.11(6).2920-25
01 June 2020
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