噻吩并[3,2-d]嘧啶衍生物的设计、合成及作为 ADAMTS-5（聚集素酶-2）抑制剂的构效关系研究。
Design, synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors.
机构信息
Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Shizuoka 410-2321, Japan.
出版信息
Bioorg Med Chem Lett. 2013 Apr 1;23(7):2111-6. doi: 10.1016/j.bmcl.2013.01.120. Epub 2013 Feb 9.
PMID:23453072
Abstract
A series of 1,1-dioxothieno[2,3-d]isothiazole (thienosultam) derivatives were designed and synthesized as novel ADAMTS-5 inhibitors for an investigation into a side chain of thienosultam for the S1' pocket. The resulting compounds (19 and 24) show high ADAMTS-5 inhibition and other MMP selectivity, and these compounds show good oral bioavailability.
摘要
设计并合成了一系列 1,1-二氧代噻吩并[2,3-d]异噻唑（噻吩并噻唑）衍生物，作为新型 ADAMTS-5 抑制剂，用于研究噻吩并噻唑的 S1' 口袋侧链。得到的化合物（19 和 24）对 ADAMTS-5 具有高抑制作用和其他 MMP 选择性，并且这些化合物具有良好的口服生物利用度。
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