3-Phenyl-5-isothiazole carboxamides with potent mglur1 antagonist activity

…, KE Garbison, JM Gruber, BA Heinz, S Iyengar…

文献索引：Fisher, Matthew J.; Backer, Ryan T.; Barth, Vanessa N.; Garbison, Kim E.; Gruber, Joseph M.; Heinz, Beverly A.; Iyengar, Smriti; Hollinshead, Sean P.; Kingston, Anne; Kuklish, Steven L.; Li, Linglin; Nisenbaum, Eric S.; Peters, Steven C.; Phebus, Lee; Simmons, Rosa Maria A.; Van Der Aar, Ellen Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2514 - 2517

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被引用次数: 8

摘要

The disclosed 3-phenyl-5-isothiazole carboxamides are potent allosteric antagonists of mGluR1 with generally good selectivity relative to the related group 1 receptor mGluR5. Pharmacokinetic properties of a member of this series (1R, 2R)-N-(3-(4-methoxyphenyl)-4- methylisothiazol-5-yl)-2-methylcyclopropanecarboxamide (14) are good, showing acceptable plasma and brain exposure after oral dosing. Oral administration of isothiazole ...