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Total Synthesis and SARS-CoV-2 3CLpro Inhibition Activities of (±)-Tuaimenal A and Its Derivatives
Zeyu Tao1, Jichen Guan1, Guangyan Zhang1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, P. R. China.
Abstract:
The first total synthesis of (±)-tuaimenal A was achieved in six steps starting from sesamol, with an overall yield of 26.4%. The key transformation was a tandem pyridine-catalyzed condensation/6π-electrocyclization sequence, which efficiently constructed the 2H-benzopyran core. Chiral resolution of the racemate was accomplished by using Boc-d-Phe-OH as a chiral auxiliary. Enzymatic inhibition assays revealed that both (+)-tuaimenal A and its enantiomer exhibited comparable inhibitory activity against SARS-CoV-2 3CLpro (the viral main protease). Furthermore, 20 analogues were synthesized, and the preliminary structure-activity relationship (SAR) was discussed.
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