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Synthesis and structure–activity relationship of tetrahydropyrazolopyrimidine derivatives—A novel structural class of potent calcium-sensing receptor antagonists

2010; Elsevier BV; Volume: 18; Issue: 24 Linguagem: Inglês

10.1016/j.bmc.2010.10.035

1464-3391

Masato Yoshida, Akira Mori, Atsuhiro Inaba, Masahiro Oka, Haruhiko Makino, Masashi Yamaguchi, Hisashi Fujita, Tomohiro Kawamoto, Mika Goto, Hiroyuki Kimura, Atsuo Baba, Tsuneo Yasuma,

Protein Kinase Regulation and GTPase Signaling

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.