Details

Autor(en) / Beteiligte

• Konkel, Michael J
• Lagu, Bharat
• Boteju, Lakmal W
• Jimenez, Hermogenes
• Noble, Stewart
• Walker, Mary W
• Chandrasena, Gamini
• Blackburn, Thomas P
• Nikam, Sham S
• Wright, Jon L
• Kornberg, Brian E
• Gregory, Tracy
• Pugsley, Thomas A
• Akunne, Hyacinth
• Zoski, Kim
• Wise, Lawrence D

Titel

3-Arylimino-2-indolones Are Potent and Selective Galanin GAL3 Receptor Antagonists

Ist Teil von

• Journal of medicinal chemistry, 2006-06, Vol.49 (13), p.3757-3758

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2006

Quelle

MEDLINE

Beschreibungen/Notizen

• A series of 3-imino-2-indolones are the first published, high-affinity antagonists of the galanin GAL3 receptor. One example, 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (9), was shown to have high affinity for the human GAL3 receptor (K i = 17 nM) and to be highly selective for GAL3 over a broad panel of targets, including GAL1 and GAL2. Compound 9 was also shown to be an antagonist in a human GAL3 receptor functional assay (K b = 29 nM).