Synthesis, Anticancer and Antibacterial Activity of Some Novel 1, 2, 4- Triazole Derivatives Containing Pyrazole and Tetrazole Rings Khanage Shantaram G.1,*, Mohite Popat B.1, Raju S. Appala2 1Department of Pharmacy, Vinayaka Missions University, Salem, Sankari main Road, NH-47, Tamilnadu, India-636308 2Department of Pharmaceutical Chemistry, H.K.E.’S College of Pharmacy, Sedam Road, Gulbarga, Karnataka, India-585105 *Corresponding Author E-mail: shantaram1982@gmail.com
Online published on 6 March, 2013. Abstract 3-methyl-pyrazol-5-one and 5-phenyl-1H-tetrazole moieties fused with substituted aryl 1, 2, 4-triazoles in a single molecular frame work were designed and synthesized to meet structural requirements essential for anticancer and antibacterial properties. 5-[3-methyl-pyrazol-5-one]-3-(Substituted Aryl)-4H-1, 2, 4 –triazole (4a-h) and of 5-[(5phenyl-1H-tetrazol-1-yl) Methyl]-3(Substituted Aryl)-4H-1, 2, 4 –triazole (8a-h) derivatives were synthesized and evaluated for anticancer and antibacterial activity. The anticancer activity of seven selected compounds from newly synthesized series were evaluated at the National Cancer Institute for testing against a panel of approximately 60 different human tumor cell lines derived from nine neoplastic cancer types. The compound 4g was found to be active anticancer agent with selective influence on renal cancer cell line UO 31 with a growth percentage of -34.97 but other compounds from series found inactive on other cancer cell lines. The in vitro antibacterial activity were tested by cup plate method against two gram positive bacteria S. aureus NCIM 2079, B. subtillis NCIM 2063 and two gram negative bacteria E. coli NCIM 2065, P. aeruginosa NCIM 2863. Compound 4a, 4b, 4d, 8a, 8b and 8d showed significant antibacterial activity against tested bacteria. Compound 4f and 8f found to be most potent antibacterial compounds in the synthesized series. Top Keywords 1,2,,4-Triazole, 3-methyl-pyrazol-5-one, 5-phenyl-1H-tetrazole, Anticancer activity, Antibacterial activity. Top |