6-苯-1H-咪唑并[4,5-c]吡啶-4-甲腈作为组织蛋白酶 S 抑制剂。
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
机构信息
Merck Research Laboratories, Newhouse, Lanarkshire ML1 5SH, UK.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17.
PMID:20598883
Abstract
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-head in comparison with the well reported pyrimidine-2-carbonitrile cysteine cathepsin inhibitors. Compound 47 is also very potent in in vivo mouse spleenic Lip10 accumulation assays.
摘要
6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈类似物被鉴定为强效和选择性组织蛋白酶 S 抑制剂，对纯化酶和人 JY 细胞基于细胞的测定均具有抑制活性。与报道的嘧啶-2-甲腈半胱氨酸组织蛋白酶抑制剂相比，该核心具有非常稳定的硫代捕获腈弹头。化合物 47 在体内小鼠脾脏 Lip10 积累测定中也非常有效。
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