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      https://www.ias.ac.in/article/fulltext/jcsc/133/0016

    • Keywords

       

      L-Proline thiourea; biscoumarin; anthelmintic; Raillietina echinobothrida; docking

    • Abstract

       

      Due to serious side effects of benzimidazoles such as apoptosis and mitotic arrest, development of alternative anthelmintic drugs with comparable efficacy to target the acetylcholine receptors of parasites is considered very important to control this parasitic disease. Here we have developed an excellent method for synthesis of biscoumarins by employing a mild and efficient proline derived bifunctional thiourea catalyst bearing pyrrolidine and thiourea catalytic sites and tested their anthelmintic activity against helminth parasites Raillietina echinobothrida and Syphacia obvelata. The compounds 2a, 2j, 2k and 2o demonstrated much stronger anthelmintic activity against Raillietina echinobothrida in comparison to the standard drug, Praziquantel. Molecular docking simulations of the optimized compounds with b-tubulin showed excellent binding interactions with several amino acid residues of the active site and the docking scores with b-tubulin were found to be comparable to the in vitro anthelmintic activity.

    • Graphical Abstract

       

      A series of biscoumarins were synthesized and they showed excellent anthelmintic properties in comparison to conventional benzimidazoles.

    • Author Affiliations

       

      BALAMPHRANG KHARRNGI1 ERRINI DECRUSE DHAR2 GRACE BASUMATARY1 DHARITRI DAS3 RAMESH CH DEKA3 ARUN K YADAV2 GHANASHYAM BEZ1

      1. Department of Chemistry, North-Eastern Hill University, Shillong, Meghalaya 793022, India
      2. Department of Zoology, North-Eastern Hill University, Shillong, Meghalaya 793022, India
      3. Department of Chemical Sciences, Tezpur University, Napaam, Tezpur, Assam 784028, India
    • Dates

       
  • Journal of Chemical Sciences | News

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