1041171-19-0Relevant articles and documents
THERAPEUTIC COMPOUNDS
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Page/Page column 120, (2010/04/27)
The invention relates to novel resolvin compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel resolvin compounds of the invention.
Synthesis and pharmacological evaluation of bis-3-(3,4-dichlorophenyl)acrylamide derivatives as glycogen phosphorylase inhibitors
Onda, Kenichi,Shiraki, Ryota,Yonetoku, Yasuhiro,Momose, Kazuhiro,Katayama, Naoko,Orita, Masaya,Yamaguchi, Tomohiko,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
experimental part, p. 8627 - 8634 (2009/04/11)
During our research using a high-throughput screening system for discovery of a new class of human liver glycogen phosphorylase a (hLGPa) inhibitors, a series of 3-(3,4-dichlorophenyl)acrylamide derivatives were synthesized, and their inhibitory activities toward hLGPa were evaluated. Among the derivatives, (2E,2′E)-N,N′-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide] (6c) inhibited hLGPa with an IC50 value of 0.023 μM. An X-ray crystallographic study of the enzyme-6c complex showed that the inhibitor is bound at the dimer interface site, where the 3,4-dichlorophenyl moiety interacts hydrophobically with the enzyme.