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Synthesis, biological evaluation and molecular docking analysis of novel benzopyrimidinone derivatives as potential anti-tyrosinase agents

Abstract : 2-substitued-benzopyrimidinones 2 were synthesized in high to excellent yields in a single step via condensation of 2-aminobenzamide 1 with some aryl-aldehydes in the presence of iodine. Cyclocondensation reaction of hydrazides 3 which were obtained in two steps from benzopyrimidinones 2, with some electrophilic species such as 2,4-pentandione, 2,5-hexandione, 1-phenylbutan-1,3-dione and cyclic anyhdrides provided the new compounds 4a–c, 5a–c, 6a–c, 7a–c, 8a–c and 9a–c. The synthesized compounds were characterized by spectroscopic means. They were also evaluated for their anti-tyrosinase potential. The structure-activity relationship (SAR) was discussed on the basis of the molecular docking analysis. © 2019
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https://hal-normandie-univ.archives-ouvertes.fr/hal-02413310
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Submitted on : Monday, December 16, 2019 - 10:45:09 AM
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Sarra Chortani, Vijaykumar D. Nimbarte, Mabrouk Horchani, Hichem Ben Jannet, Anis Romdhane. Synthesis, biological evaluation and molecular docking analysis of novel benzopyrimidinone derivatives as potential anti-tyrosinase agents. Bioorganic Chemistry, Elsevier, 2019, 92, pp.103270. ⟨10.1016/j.bioorg.2019.103270⟩. ⟨hal-02413310⟩

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