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3,4-Hydropyrimidin-2-(1H)one derivatives: solid silica-based sulfonic acid catalyzed microwave-assisted synthesis and their biological evaluation as antihypertensive and calcium channel blocking agents

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Abstract

Microwave assisted simple, efficient procedure for one-pot Biginelli condensation reaction of aldehydes, β-ketoesters, and urea or thiourea in solvent-free condition employing solid silica-based sulfonic acid as a novel, heterogeneous reusable catalyst is described. Compared to the classical Biginelli reaction conditions, the present method has the advantages of good yields, short reaction times, and experimental simplicity. The newly synthesized compounds have been screened to in vitro antihypertensive and calcium channel blocking activity done by IC50 measurement method with nifedipine as standard.

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Acknowledgments

The corresponding author is highly grateful to Madhya Pradesh Council of Science & Technology for financial support. Authors are also thankful to Deputy Director and Head, SAIF, Central Drug Research Institute (CDRI), Lucknow for providing elemental analysis and spectral data and R. V. Sree Harsha, Department of Microbiology, University of Hyderabad for providing microbiological facilities.

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Authors and Affiliations

  1. Laboratory of Heterocycles, School of Studies in Chemistry & Biochemistry, Vikram University, Ujjain, 456010, Madhya Pradesh, India

    Srinivasa Rao Jetti & Shubha Jain

  2. Department of Engineering Chemistry, Lakshmi Narain College of Technology & Science, Bhopal, 462021, Madhya Pradesh, India

    Amitbodh Upadhyaya

Authors
  1. Srinivasa Rao Jetti
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  2. Amitbodh Upadhyaya
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  3. Shubha Jain
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Correspondence to Srinivasa Rao Jetti.

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Jetti, S.R., Upadhyaya, A. & Jain, S. 3,4-Hydropyrimidin-2-(1H)one derivatives: solid silica-based sulfonic acid catalyzed microwave-assisted synthesis and their biological evaluation as antihypertensive and calcium channel blocking agents. Med Chem Res 23, 4356–4366 (2014). https://doi.org/10.1007/s00044-014-0988-y

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  • DOI: https://doi.org/10.1007/s00044-014-0988-y

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