Main Article Content
Abstract
The present work describes the synthesis and biological evaluation of substituted 1,2,4-triazole derivatives. Synthesis is carried out by the condensation reaction of benzothiamide derivative with 2,2,2-trifluoroacetohydrazide to give 1,2,4-triazole, which was further modified by N-alkylation and Suzuki– Miyaura coupling reaction. Furthermore, the characterization of the product is carried out by elemental analysis and spectral analysis. Products were evaluated for their in vitro biological assay for antibacterial activity against various bacterial standard strains, i.e. Staphylococcus aureus MTCC-96, Streptococcus pyogenes-MTCC-443, two Gram-negative bacteria Escherichia coli MTCC-442, Pseudomonas aeruginosa-MTCC-441 and three fungal strains Candida albicans MTCC-227, Aspergillus niger MTCC- 282, Aspergillus clavatus MTCC-1323 at different concentrations and the results were compared with standard drugs.
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References
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References
R.J. Singh and D.K. Singh, E-J.Chem., 7, 37 (2010); https://doi.org/10.1155/2010/168651.
C.T. Supuran, Curr. Pharm. Des., 14, 641 (2008); https://doi.org/10.2174/138161208783877947.
L.-Z. Xu, S.-S. Zhang, Z.-Q. Hu and K. Jiao, Chem. Res. Chin. Univ., 19, 310 (2003).
S.C. Holm and B.F. Straub, Org. Prep. Proc. Int., 43, 319 (2009); https://doi.org/10.1080/00304948.2011.593999.
J.W. Hull Jr., D.R. Romer, T.J. Adaway and D.E. Podhorez, Org. Process Res. Dev., 13, 1125 (2009); https://doi.org/10.1021/op9001577.
I.S. Churilov, S.V. Popkov, A.A. Grishina, E.V. Chembarova and O.Y. Mironova, Chem. Ind. Today, 8, 31 (2008).
A.I. Matesanz, C. Joie and P. Souza, Dalton Trans., 39, 7059 (2010); https://doi.org/10.1039/c003007d.
T. Mano, R.W. Stevens, Y. Okumura, M. Kawai, T. Okumura and M. Sakakibara, Bioorg. Med. Chem. Lett., 15, 2611 (2005); https://doi.org/10.1016/j.bmcl.2005.03.041.
S.M. Rida, S.A. El-Hawash, H.T. Fahmy, A.A. Hazzaa and M.M. El-Meligy, Arch. Pharm. Res., 29, 826 (2006); https://doi.org/10.1007/BF02973901.
W.F. van Der Meide, L.O. Sabajo, A.J. Jensema, I. Peekel, W.R. Faber, H.D. Schallig and R.F. Fat, Int. J. Dermatol., 48, 52 (2009); https://doi.org/10.1111/j.1365-4632.2009.03883.x.
G. Qian, Z. Chun-ling, F. Wei-wei and F. Ju-Zheng, Huaxi Yaoxue Zazhi, 24, 475 (2009).
B.S. Holla, B. Veerendra, M. Shivananda and B. Poojary, Eur. J. Med. Chem., 38, 759 (2003); https://doi.org/10.1016/S0223-5234(03)00128-4.
M. Groessl, E. Reisner, C.G. Hartinger, R. Eichinger, O. Semenova, A.R. Timerbaev, M.A. Jakupec, V.B. Arion and B.K. Keppler, J. Med. Chem., 50, 2185 (2007); https://doi.org/10.1021/jm061081y.
C. Dahlof and C. Lines, Expert Opin. Investig. Drugs, 8, 671 (1999); https://doi.org/10.1517/13543784.8.5.671.
National Committee for Clinical and Laboratory Standards, Method for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically Approved Standard, NCCLS, Villanova, Italy, edn 4, Document M 100-S7. S100-S157 (1997).
D.H. Isenberg, Essential Procedure for Clinical Microbiology, American Society for Microbiology, Washington (1998).
J.R.Zgoda and J.R.Porter, Pharm. Biol., 39, 221 (2001); https://doi.org/10.1076/phbi.39.3.221.5934.