Development of 4-aminoquinoline-1,3,5-triazine conjugates as potent antibacterial agent through facile synthetic route
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Med Chem Res DOI 10.1007/s00044-013-0521-8
ORIGINAL RESEARCH
Development of 4-aminoquinoline-1,3,5-triazine conjugates as potent antibacterial agent through facile synthetic route Hans Raj Bhat • Pankaj Kumar Pandey • Surajit Kumar Ghosh • Udaya Pratap Singh
Received: 15 October 2012 / Accepted: 29 January 2013 Ó Springer Science+Business Media New York 2013
Abstract A series of novel hybrid 4-aminoquinoline-1,3,5triazine derivatives were developed and subsequently tested against representative Gram-positive and Gram-negative microorganisms for determination of their antibacterial activity. Screening results indicate that, title molecule exhibit moderate to potent activity in comparison to standard. These hybrid derivatives were synthesized through a facile synthetic routes and structure of reaction intermediates as well as target molecules were recognised with the aid of various spectroscopic techniques viz., FTIR, NMR, mass and elemental analysis. Keywords 1,3,5-Triazine 4-Aminoquinoline Antibacterial Introduction The emergence of multi-drug resistance (MDR) pathogens in last decades significantly jeopardises the global healthElectronic supplementary material The online version of this article (doi:10.1007/s00044-013-0521-8) contains supplementary material, which is available to authorized users. H. R. Bhat (&) P. K. Pandey U. P. Singh Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture Technology & Sciences, Formerly Allahabad Agricultural Institute, Deemed to be University, Allahabad 211007, India e-mail: [email protected] S. K. Ghosh Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786004, Assam, India Present Address: U. P. Singh Archimedes DoRa5 Fellow, Division of Bioorganic Chemistry, Institute of Chemistry, University of Tartu, Tartu, Estonia
care system in both poor and developed countries (Alanis, 2005; Shapiro et al., 2011). Whereas, non-judicious use of these drugs has contributed largely among the other factors that brought up the mutation in microbial genome (Martinez and Baquero, 2000). This has put a selective pressure and necessitates the discovery of novel antimicrobial agents that acted via a novel pathway (Davies and Davies, 2010). The 1,3,5-triazine scaffold has provided the basis for the design of biologically significant molecules with diverse therapeutic profile, e.g. as antifungal (Singh et al., 2012a, 2013a), anticancer (Corbett et al., 1982), antimalarial (Bhat et al., 2011, 2012a, 2013), antiviral (Lozano et al., 2011) and antibacterial activity (Gahtori et al., 2012). In continuation of our project (Junejo et al., 2011), till now, we had reported numerous antibacterial hybrid conjugates of 1,3,5triazine with thiazole (Singh et al., 2011), piperazine (Ghosh et al., 2012), 4-aminoquinoline (Bhat et al., 2012b) and 1,3,4-thiadiazole (Dubey et al., 2012), thiazolidine-4one (Kumar et al., 2013) as potent antimicrobial compounds. In our recent communication, inhibition of bacterial translation was identified as mechanism of
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