Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376976 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael J. Konkel, Mathivanan Packiarajan, Heidi Chen, Upendra P. Topiwala, Hermogenes Jimenez, Ian Jamie Talisman, Heather Coate, Mary W. Walker,