94102-85-9Relevant academic research and scientific papers
Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors
Tsukada, Tomoharu,Takahashi, Mizuki,Takemoto, Toshiyasu,Kanno, Osamu,Yamane, Takahiro,Kawamura, Sayako,Nishi, Takahide
scheme or table, p. 1004 - 1007 (2010/06/16)
With the goal of improving metabolic stability and further enhancing FBPase inhibitory activity, a series of tricyclic 8H-indeno[1,2-d][1,3]thiazoles was designed and synthesized with the aid of structure-based drug design. Extensive SAR studies led to th
Discovery of potent and orally active tricyclic-based FBPase inhibitors
Tsukada, Tomoharu,Kanno, Osamu,Yamane, Takahiro,Tanaka, Jun,Yoshida, Taishi,Okuno, Akira,Shiiki, Takeshi,Takahashi, Mizuki,Nishi, Takahide
experimental part, p. 5346 - 5351 (2010/09/05)
With the aim of exploring the effect of tricyclic-based FBPase inhibitors in cells and in vivo, a series of prodrugs of tricyclic phosphonates was designed and synthesized. Introducing prodrug moieties into tricyclic-based phosphonates led to the discover
Method and composition for treatment of inflammatory bowel disease
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, (2008/06/13)
A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a pharmaceutically acceptable carrier therefor. Also disclosed is a method for
Method and composition for treatment of inflammatory bowel disease
-
, (2008/06/13)
A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a pharmaceutically acceptable carrier therefor. Also disclosed is a method for
Desazadesmethyldesferrithiocin analogues as orally effective iron chelators
Bergeron, Raymond J.,Wiegand, Jan,Weimar, William R.,Vinson, J. R. Timothy,Bussenius, J?rg,Yao, Guo Wei,McManis, James S.
, p. 95 - 108 (2007/10/03)
Further structure-activity studies of desferrithiocin analogues are carried out. (S)-Desazadesmethyldesferrithiocin, 2-(2-hydroxyphenyl)-Δ2- thiazoline-4(S)-carboxylic acid, serves as the principal framework in the current paper. Desazadesmethyldesferrithiocin can be structurally altered with facility, and data are already available on its iron-clearing properties and toxicity parameters. Four different kinds of structural modifications of this framework are undertaken: introduction of hydroxy, carboxy, or methoxy groups on the aromatic ring; alteration of the thiazoline ring; increasing the distance between the ligand donor atoms; and benz-fusion of the aromatic rings. The structural modifications described are shown to have a tremendous impact on both the iron clearance and toxicity profiles of the desazadesmethyldesferrithiocin molecule. All of the compounds are assessed in a bile-duct-cannulated rodent model to determine iron clearance efficiency. Ligands which demonstrate an efficiency of greater than 2% are carried forward to the iron-overloaded primate for iron-clearing measurements. Ligands with efficiencies greater than 3% in the primate are then evaluated in a formal toxicity study in rodents. On the basis of the results of the present work, 2-(2,4-dihydroxyphenyl)-Δ2-thiazoline-4(S)-carboxylic acid is a promising candidate for clinical evaluation.
