• ARUN K YADAV

      Articles written in Journal of Chemical Sciences

    • Coumarin-based Trisubstituted Methanes as Potent Anthelmintic: Synthesis, Molecular Docking and in vitro Efficacy

      GRACE BASUMATARY ERRINI DECRUSE DHAR DHARITRI DAS RAMESH CH DEKA ARUN K YADAV GHANASHYAM BEZ

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      A series of coumarin-based trisubstituted methanes (TRSMs) having uracil scaffold was synthesised employing a green, chromatography-free, and a highly efficient sonochemical multicomponent reaction of diverse aldehydes with 1,3-dimethyl-6-aminouracil and 4-hydroxy-coumarin in the presence of acatalytic amount of DABCO at room temperature and tested their anthelmintic efficacy against helminth parasites, Raillietina echinobothrida and Syphacia obvelata. Some of the TRSMs with substituents in the para position of the phenyl ring showed excellent anthelmintic activity in comparison to the commonly used drugs such as albendazole and praziquantel. The docking study revealed the binding interaction of all the optimizedcompounds with several amino acid residues in the active site of b-tubulin. The compounds showing gooddocking score with b-tubulin showed comparable anthelmintic activity experimentally as well.

    • Developing a highly potent anthelmintic: study of catalytic application of L-proline derived aminothiourea in rapid synthesis of biscoumarins and their in vitro anthelmintic essay

      BALAMPHRANG KHARRNGI ERRINI DECRUSE DHAR GRACE BASUMATARY DHARITRI DAS RAMESH CH DEKA ARUN K YADAV GHANASHYAM BEZ

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      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.

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

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