Affiliations 

  • 1 Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan
  • 2 Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan. zubairmkn@yahoo.com
  • 3 Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan. nasirhej@yahoo.co.uk
  • 4 Department of Chemistry, COMSATS Institute of Information Technology, University Road, Tobe Camp, Abbottabad, 22060, Pakistan
  • 5 Deparment of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Science, University Putra Malaysia, 43400, Serdang, Selangor Darul Ehsan, Malaysia. noorjahan@upm.edu.my
  • 6 Deparment of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Science, University Putra Malaysia, 43400, Serdang, Selangor Darul Ehsan, Malaysia
  • 7 Faculty of Industrial Sciences & Technology, University Malaysia Pahang, Lebuhraya Tun Razak, 26300, Kuantan, Pahang, Malaysia
  • 8 Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur, 63000, Pakistan
  • 9 HEJ Research Institute of Chemistry, International Centre for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan
Chem Cent J, 2018 May 04;12(1):49.
PMID: 29728881 DOI: 10.1186/s13065-018-0404-7

Abstract

Thiophene derivatives have shown versatile pharmacological activities. The Suzuki reaction proved a convenient method for C-C bond formations in organic molecules. In the present research work novel derivatives of 2,5-dibromo-3-methylthiophene (3a-k and 3l-p) has been synthesized, via Suzuki coupling reaction in low to moderate yields. A wide range of functional groups were well tolerated in reaction. Density functional theory investigations on all synthesized derivatives (3a-3p) were performed in order to explore the structural properties. The pharmaceutical potential of synthesized compounds was investigated through various bioassays (antioxidant, antibacterial, antiurease activities). The compounds 3l, 3g, 3j, showed excellent antioxidant activity (86.0, 82.0, 81.3%), respectively by scavenging DPPH. Synthesized compounds showed promising antibacterial activity against tested strains. 3b, 3k, 3a, 3d and 3j showed potential antiurease activity with 67.7, 64.2, 58.8, 54.7 and 52.1% inhibition at 50 µg/ml. Results indicated that synthesized molecules could be a potential source of pharmaceutical agents.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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