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• W2886783313 abstract "Abstract To explore the potential of aporphine alkaloids, a novel series of functionalized aporphine analogues with alkoxy (OCH 3 , OC 2 H 5 , OC 3 H 7 ) functional groups at C1/C2 of ring A and an acyl (COCH 3 and COPh) or phenylsulfonyl (SO 2 Ph and SO 2 C 6 H 4 ‐3‐CH 3 ) functionality at the N6 position of ring B of the aporphine scaffold were synthesized and evaluated for their arachidonic acid (AA)‐induced antiplatelet aggregation inhibitory activity and 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) free‐radical‐scavenging antioxidant activity, with acetylsalicylic acid and ascorbic acid as standard references, respectively. The preliminary structure–activity relationship related to AA‐induced platelet aggregation inhibitory activity results showed that the aporphine analogues 1‐[1,2,9,10‐tetramethoxy‐6 a ,7‐dihydro‐4 H ‐dibenzo[ de , g ]quinolin‐6(5 H )‐yl]ethanone and 1‐[2‐(benzyloxy)‐1,9,10‐trimethoxy‐6 a ,7‐dihydro‐4 H ‐dibenzo[ de , g ]quinolin‐6(5 H )‐yl]ethanone to be the best compounds of the series. Moreover, the DPPH free‐radical‐scavenging antioxidant activity results demonstrated that the aporphine analogues 1,2,9,10‐tetramethoxy‐6‐(methylsulfonyl)‐5,6,6 a ,7‐tetrahydro‐4 H ‐dibenzo[ de , g ]quinoline, 2‐ethoxy‐1,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6 a ,7‐tetrahydro‐4 H ‐dibenzo[ de , g ]quinoline, 1‐ethoxy‐2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6 a ,7‐tetrahydro‐4 H ‐dibenzo[ de , g ]quinoline, 2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐1‐propoxy‐5,6,6 a ,7‐tetrahydro‐4 H ‐dibenzo[ de , g ]quinoline, and 1‐(benzyloxy)‐2,9,10‐trimethoxy‐6‐(methylsulfonyl)‐5,6,6 a ,7‐tetrahydro‐4 H ‐dibenzo[ de , g ]quinoline were the best compounds of the series. Moreover, in silico molecular docking simulation studies of the active analogues were also performed." @default.
• W2886783313 created "2018-08-22" @default.
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• W2886783313 date "2018-08-08" @default.
• W2886783313 modified "2023-10-17" @default.
• W2886783313 title "Discovery of Aporphine Analogues as Potential Antiplatelet and Antioxidant Agents: Design, Synthesis, Structure–Activity Relationships, Biological Evaluations, and in silico Molecular Docking Studies" @default.
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• W2886783313 doi "https://doi.org/10.1002/cmdc.201800318" @default.
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