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Design, synthesis and pharmacological analysis of 5-[4′-(substituted-methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles

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Abstract

In the present paper 5-[4′-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles (5a–g) and [2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h–q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses. Some of the compounds have shown significant pharmacological properties.

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Acknowledgements

The authors acknowledge BioGenics, Hubballi for carrying out ACE-inhibition activity and National Cancer Institute, NIH, Bethesda, USA for anti-proliferative activity analyses under DTP Program. The authors are also grateful to authorities of Dr. Prabhakar Kore Basic Science Research Centre Belgaum, Karnataka, India for anti-inflammatory and antifungal activity assay. The authors wish to thank the University Scientific Instrumentation Centre (USIC), Karnataka University, Dharwad, NMR Research Centre, Indian Institute of Science (IISc), Bengaluru, India for carrying out the spectral analyses. Authors also thank University Grants Commission, New Delhi for providing financial assistants under DSA: F-540/2/DSA/2013(SAP-I), UGC-UPE “Antitumor activity: An Integrated Approach” vide F. No. 14-3/2012 (NS/PE).

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Authors and Affiliations

  1. Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, Karnataka, 580003, India

    Atulkumar Kamble, Ravindra Kamble & Mahadev Kumbar

  2. Dr. Prabhakar Kore Basic Science Research Center, KLE University, Belagavi, Karnataka, 590010, India

    Suneel Dodamani, Sunil Jalalpure & Vijaykumar Rasal

  3. KLE University’s College of Pharmacy, Belagavi, Karnataka, 590010, India

    Sunil Jalalpure & Vijaykumar Rasal

  4. Soniya Education Trust’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad, Karnataka, 580002, India

    Shrinivas Joshi & Sheshagiri Dixit

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  1. Atulkumar Kamble
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Kamble, A., Kamble, R., Dodamani, S. et al. Design, synthesis and pharmacological analysis of 5-[4′-(substituted-methyl)[1,1′-biphenyl]-2-yl]-1H-tetrazoles. Arch. Pharm. Res. 40, 444–457 (2017). https://doi.org/10.1007/s12272-017-0887-0

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