Design, synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors
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 AD
A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mamma
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Page/Page column 102
(2009/08/14)
Thienithiazine derivatives
Thienothiazine derivatives of the formula STR1 are provided. These derivatives are useful for the treatment of inflammation and pain.
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(2008/06/13)
Thiophene isosteres: synthesis and pharmacological study of 3-(azol-1-yl)thieno isothiazole-1,1-dioxides
Three series of new 3-(azol-1-yl)thieno isothiazole-1,1-dioxides were synthesized and tested for anti-inflammatory and related pharmacological activities as well as for acute toxicity.Acetylsalicylic acid was used as the reference standard.Keywords - 3-(a
Vega, Salvador,Madronero, Ramon,Diaz, J. Antonio,Junquera, Francisco,Alonso, Javier,et al.
p. 329 - 334
(2007/10/02)
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