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Discovery of selective PDE4B inhibitors.
TLDR
The first PDE4B selective inhibitor is described, which exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast. Expand
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
A series of thiazole bearing thiazolidin-4-one was discovered via high-throughput screening as non-competitive inhibitors of ADAMTS-5. Compound 31 appeared to give the best ADAMTS-5 inhibition andExpand
Design, synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors.
TLDR
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, and these compounds show good oral bioavailability. Expand
DOUBLE COORDINATION ABILITY OF BIS(DIMETHYLALUMINUM) SULFATE TOWARD CARBONYL SUBSTRATES
Abstract New insight into the crucial role of bis(dimethylaluminum) sulfate as bidentate Lewis acid has been demonstrated using typical carbonyl allylation and Diels-Alder reaction in comparison withExpand