- 4H-THIENO[3,2-C]CHROMENE-BASED INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE
-
Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
- -
-
Page/Page column 18
(2012/12/13)
-
- Synthesis, SAR, and X-ray structure of tricyclic compounds as potent FBPase inhibitors
-
With the aim of discovering a novel class of fructose-1,6-bisphosphatase (FBPase) inhibitors, a series of compounds based on tricyclic scaffolds was synthesized. Extensive SAR studies led to the finding of 8l with an IC50 value of 0.013 μM against human FBPase. An X-ray crystallographic study revealed that 8l bound at AMP binding sites of human liver FBPase with hydrogen bonding interactions similar to AMP.
- Tsukada, Tomoharu,Takahashi, Mizuki,Takemoto, Toshiyasu,Kanno, Osamu,Yamane, Takahiro,Kawamura, Sayako,Nishi, Takahide
-
scheme or table
p. 5909 - 5912
(2010/04/30)
-
- A ring expansion strategy in antiviral synthesis: A novel approach to TAK-779
-
A synthesis of TAK-779 that relies on construction of a key carboxylic acid intermediate by a ring expansion with TMSCHN2 is described.
- Smalley Jr., Terrence L.
-
p. 1973 - 1980
(2007/10/03)
-
- AMINO ACID DERIVATIVE
-
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): STR1 wherein R 1 represents a hydrogen atom or an acyl group; R 2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.
- -
-
-
- Synthesis of Benzoic and Tetralone Carboxylic Acid Esters from Phenols by Palladium Catalyzed Alkoxy/Aryloxy Carbonylation
-
Various phenols with an acyl group conjugated to the aromatic system were converted via trifluoromethanesulfonates into benzoic acid esters by a palladium catalyzed alkoxy/aryloxy carbonylation.
- Gerlach, Uwe,Wollmann, Theo
-
p. 5499 - 5502
(2007/10/02)
-
