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Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.
Shiozaki, Makoto; Imai, Hiroto; Maeda, Katsuya; Miura, Tomoya; Yasue, Katsutaka; Suma, Akira; Yokota, Masahiro; Ogoshi, Yosuke; Haas, Julia; Fryer, Andrew M; Laird, Ellen R; Littmann, Nicole M; Andrews, Steven W; Josey, John A; Mimura, Takayuki; Shinozaki, Yuichi; Yoshiuchi, Hiromi; Inaba, Takashi.
Afiliação
  • Shiozaki M; Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan. makoto.shiozaki@ims.jti.co.jp
Bioorg Med Chem Lett ; 19(21): 6213-7, 2009 Nov 01.
Article em En | MEDLINE | ID: mdl-19767207
ABSTRACT
A series of 1-sulfonylaminocyclopropanecarboxylates was synthesized as ADAMTS-5 (Aggrecanase-2) inhibitors. After an intensive investigation of the central cyclopropane core including its absolute stereochemistry and substituents, we found compound 22 with an Agg-2 IC50=7.4 nM, the most potent ADAMTS-5 inhibitor reported so far.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Sulfonamidas / Ciclopropanos / Proteínas ADAM Idioma: En Ano de publicação: 2009 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Sulfonamidas / Ciclopropanos / Proteínas ADAM Idioma: En Ano de publicação: 2009 Tipo de documento: Article