Title of article
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport
Author/Authors
Bradford H. Hirth، نويسنده , , Shuang Qiao، نويسنده , , Lisa M. Cuff، نويسنده , , Brian M. Cochran، نويسنده , , Marko J. Pregel، نويسنده , , Jill S. Gregory، نويسنده , , Scott F. Sneddon، نويسنده , , John L. Kane Jr.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
2087
To page
2091
Abstract
A series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase chloride transport in cells expressing mutant cystic fibrosis transmembrane conductance regulator (CFTR) protein has been identified from our compound library. Analoging efforts and the resulting structure–activity relationships uncovered are detailed. Compound potency was improved over 30-fold from the original lead, yielding several analogs with EC50 values below 10 nM in our cellular chloride transport assay.
Keywords
CFTR , cystic fibrosis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795537
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