Synthesis and antimicrobial evaluation of novel substituted pyrimidine scaffold
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Med Chem Res DOI 10.1007/s00044-013-0596-2
ORIGINAL RESEARCH
Synthesis and antimicrobial evaluation of novel substituted pyrimidine scaffold Hardik B. Ghodasara • Amit R. Trivedi Vipul B. Kataria • Bharat G. Patel • Viresh H. Shah
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Received: 10 May 2012 / Accepted: 24 April 2013 Ó Springer Science+Business Media New York 2013
Abstract Synthesis and biological evaluation of substituted pyrimidine derivatives containing 4-amino and 5-cyano substituted derivatives are described. Biginelli typed three component reactions between an aldehyde, malononitrile, and a urea constituent give a rapid facile pyrimidine ring. The constitution of the products has been delineated by elemental analysis and spectral analysis. The products were assayed for their in vitro biological assay antibacterial activity against S. pyogenes MTCC-442, S. aureus MTCC-96, E. coli MTCC-443, and B. subtilis MTCC-441 bacterial strain and antifungal activity against Aspergillus niger MTCC-282 and Candida albicans MTCC-227 at different concentrations, which compared with Ampicillin, Chloramphenicol, Ciprofloxacin, Norfloxacin, and Griseofulvin as standard drug which are presented. Keywords Pyrimidine Antibacterial Antifungal Biological assay
H. B. Ghodasara A. R. Trivedi V. B. Kataria B. G. Patel V. H. Shah (&) Department of Chemistry, Saurashtra University, Rajkot 360005, India e-mail: [email protected] H. B. Ghodasara e-mail: [email protected] A. R. Trivedi e-mail: [email protected] V. B. Kataria e-mail: [email protected] B. G. Patel e-mail: [email protected]
Introduction Heterocyclic scaffolds are of immense biological interest due to their potential physical and chemical properties (Brown, 1998). Among these groups, the pyrimidine compounds occupy a specific position in pharmaceutical chemistry, as they are components of nucleic acids. Over many years, there has been an interest in the chemistry of pyrimidine because of their biological significance. Pyrimidine and their derivatives are acknowledged to be important for drugs (Qingyun et al., 2011) and agricultural chemicals (Harkness and Wells, 1981). Pyrimidine analogous possess several interesting biological activities such as antimicrobial (Padhy et al., 2003; Bakavoli et al., 2010), antitumor (Raic´-Malic´ et al., 2000), antiviral (Ramiz et al., 2011), hypnotic, sedative (Shaabani et al., 2007), and anticonvulsant activities (Powers et al., 1980). Many pyrimidine derivatives are used for thyroid drugs (Williams and Kay, 1947) and leukemia (Raffa et al., 2004). During the last two decades, several pyrimidine derivatives have been developed as chemotherapeutic agents (Christopherson and Lyons, 1990) and have found wide medicinal applications such as antiinflammatory (Bekhit et al., 2003), diuretic (Monge et al., 1989), antimalarial (Deng et al., 2010), and cardiovascular (Kappe and Kappe, 1991). Various suitably functionalized pyrimidine derivatives show good antimycotic activity (Agarwal et al., 2000). Some pyrimidine derivatives are good antibacterial
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