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Synthesis of novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest: a 3D-QSAR study on their cytotoxicity

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Abstract

We report a library consisting of some novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest as well as their synthesis and analysis. The important steps in the synthetic part were found to be Hantzsch and Biginelli multicomponent reactions. The synthesized compounds were screened for their in vitro antibacterial activity against two gram-positive bacteria: Staphylococcus aureus and Bacillus subtilis. The title compounds did not exhibit potential antibacterial activity. Furthermore, compounds were subjected to in vitro cytotoxicity against Vero cells. Compounds exhibited weak, moderate, or high cytotoxicity. Compounds 4a, 4b, 4c, 4f, 4g, 4h, 4i, 7i, 7l, 7m, and 7r exhibited potential cytotoxicity. CoMFA study has resulted in the identification of structural features contributing toward their cytotoxicity.

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund, TN, 643 001, India

    B. R. Prashantha Kumar, Pankaj Masih & E. Karthikeyan

  2. Department of Biotechnology, JSS College of Pharmacy, Ootacamund, TN, 643 001, India

    Ankur Bansal,  Suja & Pottekad Vijayan

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  1. B. R. Prashantha Kumar
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  2. Pankaj Masih
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  3. E. Karthikeyan
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  4. Ankur Bansal
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  5. Suja
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Correspondence to B. R. Prashantha Kumar.

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Prashantha Kumar, B.R., Masih, P., Karthikeyan, E. et al. Synthesis of novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest: a 3D-QSAR study on their cytotoxicity. Med Chem Res 19, 344–363 (2010). https://doi.org/10.1007/s00044-009-9195-7

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  • DOI: https://doi.org/10.1007/s00044-009-9195-7

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