Design,synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors |
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| Authors: | Masakazu Atobe Naomi Maekawara Masashi Kawanishi Hiroko Suzuki Eiichi Tanaka Shiro Miyoshi |
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| Institution: | Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan |
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| Abstract: | A series of 1,1-dioxothieno2,3-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. |
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