Special Issue on Benzopyrazines: Synthesis, Characterization and Evaluation as Aldose Reductase Inhibitors

Submission Deadline: Mar. 10, 2020

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This special issue currently is open for paper submission and guest editor application.

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Special Issue Flyer (PDF)
  • Lead Guest Editor
    • Huma Bhatti
      Department of Chemistry, University of Karachi, Karachi, Pakistan
  • Guest Editor
    Guest Editors play a significant role in a special issue. They maintain the quality of published research and enhance the special issue’s impact. If you would like to be a Guest Editor or recommend a colleague as a Guest Editor of this special issue, please Click here to complete the Guest Editor application.
    • Syed Kashif Ali
      Department of Chemistry, University of Karachi, Karachi, Pakistan
    • Abdul Hameed
      Department of Chemistry, Forman Chiristan College, Lahore, Pakistan
    • Dr Ghulam Abbas
      Department of Pharmacology, Zia Uddin Medical University, Karachi, Pakistan
    • Jamseed Iqbal
      Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad, Pakistan
    • Syed Tariq Ali
      Department of Chemistry, Karachi University, Karachi, Pakistan
    • Nizam Uddin
      Department of Chemistry, Karachi University, Karachi, Pakistan
  • Introduction

    The synthetic route to synthesize desired benzopyrazines has been present in Scheme-1. In the first step, the α-methyl group of acetophenone was oxidized to carbonyl group by using selenium dioxide. The dicarbonyl intermediate 4 was then reacted without purification with 4-methylbenzene-1,2-diamine at room temperature to afford corresponding benzopyrazine (Scheme-1). Following the optimized method, a range of novel benzopyrazines has been prepared (Shah, et al., 2010, Wang, et al., 2009). 1H NMR spectra of the resulting products showed two regio-isomers in 1:1 to 1:0.5 ratio due to difference in reactivity of C-2 keto and C-3 aldehyde moieties in intermediate 4. The structure of two regio-isomers were fully characterize by 1H and 13C NMR two dimensional NMR techniques including COSY, NOESY, HSQC, and HMBC. Regio-isomers separation was proved to be difficult in different solvent systems. Only an isomer of 3'-bromo benzopyrazine 6i' was isolated that help to assign the structure of regioisomers from NMR data.
    In this study, we synthesized sixteen benzopyrazine derivatives and screen evaluated them against ARL2 as well as ALR1 for selectivity purpose.
    Aims and Scope:
    1. Role of aldose reductase (ALR2) in diabetic complications
    2. (16) methyl benzopyrazines were screened against aldose reductase
    3. 3'-hydroxyphenyl benzopyrazine 6l was found most active (IC50 = 1.34 ± 0.07 µM)
    4. 3'-bromophenyl analogue 6i showed comparable activity for ALR2
    5. Polyol pathway
    6. Benzopyrazines as aldose inhibitors

  • Guidelines for Submission

    Manuscripts can be submitted until the expiry of the deadline. Submissions must be previously unpublished and may not be under consideration elsewhere.

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  • Published Papers

    The special issue currently is open for paper submission. Potential authors are humbly requested to submit an electronic copy of their complete manuscript by clicking here.