Title of article
Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility
Author/Authors
Michael J. Konkel، نويسنده , , Mathivanan Packiarajan، نويسنده , , Heidi Chen، نويسنده , , Upendra P. Topiwala، نويسنده , , Hermogenes Jimenez، نويسنده , , Ian Jamie Talisman، نويسنده , , Heather Coate، نويسنده , , Mary W. Walker، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
3950
To page
3954
Abstract
A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (1) were synthesized to improve aqueous solubility, while retaining high affinity for the human galanin Gal3 receptor. A very potent analog (9e, 1,3-dihydro-1-[3-(2-pyrrolidinylethoxy)phenyl]-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one, Ki = 5 nM) shows good selectivity and solubility of 48 μg/mL at pH 7.4.
Keywords
Gal3 antagonist , galanin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797111
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