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Published on: May 24, 2024
Synthesis and structure-activity relationship of tetrahydropyrazolopyrimidine derivatives--a novel structural class
Masato Yoshida1, Akira Mori, Atsuhiro Inaba
1Pharmacutical Research Division, Takeda Pharmaceutical Company Limited, 17-85, Jusohonmachi-2-chome, Yodogawa-ku, Osaka 532-8686, Japan. Yoshida_Masato@takeda.co.jp
Abstract:
A series of novel tetrahydropyrazolopyrimidine derivatives containing an adamantyl group were synthesized and evaluated as potential calcium-sensing receptor (CaSR) antagonists. After chemical modification of 9a, which was identified as a hit compound in a random screening of CaSR antagonist assay, 7,7-dimethyl derivative 16c was found to be the most active compound of this new series (IC(50)=10nM). We report the synthesis of this series and their biological activities and structure-activity relationship.
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