Divergent Synthesis and Evaluation of Inhibitory Activities against Cyclooxygenases-1 and -2 of Natural Withasomnines and Analogues
スポンサーリンク
概要
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The divergent synthesis of natural withasomnines and analogues was achieved from 4-hydroxypyrazoles, which was prepared via alkaline hydrolysis of the Baeyer–Villiger oxidation products from 4-formylpyrazoles. Key steps of this synthesis are regioselective Claisen rearrangement of 4-allyloxypyrazoles and the Suzuki–Miyaura coupling of 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl trifluoromethanesulfonate and commercially available arylboronic acids. The Suzuki–Miyaura coupling at the final step of this strategy enabled facile access to natural withasomnines and their analogues. The biological activities of the twelve synthesized compounds against cyclooxygenases-1 and -2 (COX-1 and COX-2) were evaluated.
著者
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Shibano Makio
Laboratory Of Pharmacognostical Sciences Osaka University Of Pharmaceutical Sciences
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Shibano Makio
Laboratory of Pharmacognosy, Osaka University of Pharmaceutical Sciences
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Usami Yoshihide
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Watanabe Ryo
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Fujino Yuiko
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Ishida Chihiro
Laboratory of Pharmacognosy, Osaka University of Pharmaceutical Sciences
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Yoneyama Hiroki
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Harusawa Shinya
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Ichikawa Hayato
Laboratory of Pharmaceutical Organic Chemistry, Osaka University of Pharmaceutical Sciences
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Watanabe Ryo
Laboratory of Medicinal Pharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, Japan
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