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Synthesis, biological evaluation of 2,3-disubstituted-imidazolyl/benzimidazolyl-quinazolin-4(3H)-one derivatives

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Abstract

A series of disubstituted-quinazolin-4(3H)-ones derivatives have been synthesized and confirmed through IR, 1H- and 13C-NMR, MS spectroscopy and elemental analysis. Synthesized compounds were screened for in vitro and in vivo anti-inflammatory using human red blood cell membrane stabilization method and carrageenan-induced rat paw edema. The antimicrobial potency was measured by disk diffusion method. The compounds with imidazole (3g) and benzimidazole nucleus (4b and 4f) displayed a significant anti-inflammatory activity by in vitro method. Moreover, the compounds 3d and 4a exhibited a significant anti-inflammatory activity in vivo. The compounds 3d, 3f and 4g were found to be active antimicrobial agents, when compared with reference drug ciprofloxacin and amphotericin B. Thus, these compounds can serve as promising leads for further biological studies.

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Acknowledgments

The authors thank SAIF, IIT, Madras, for the NMR and GCMS spectra. Author DAP is thankful to Dr. U.K. Patil, Manish and Mahesh. This author is grateful for the blessings of the late Prof. Dr. R.A. Fursule.

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Authors and Affiliations

  1. H. R. Patel Institute of Pharmaceutical Education and Research, Karwand Naka, Dist-Dhule, Shirpur, Maharashtra, 425 405, India

    Dilip A. Patil

  2. R. C. Patel Institute of Pharmaceutical Education and Research, Karwand Naka, Dist-Dhule, Shirpur, Maharashtra, 425 405, India

    Sanjay J. Surana

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Correspondence to Dilip A. Patil.

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All applicable international, national and/or institutional guidelines for the care and use of animals were followed. This article does not contain any studies with human participants performed by any of the authors.

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Patil, D.A., Surana, S.J. Synthesis, biological evaluation of 2,3-disubstituted-imidazolyl/benzimidazolyl-quinazolin-4(3H)-one derivatives. Med Chem Res 25, 1125–1139 (2016). https://doi.org/10.1007/s00044-016-1552-8

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