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1. Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.

Author

Hirth BH, Qiao S, Cuff LM, Cochran BM, Pregel MJ, Gregory JS, Sneddon SF, and Kane JL Jr

Subjects
Amides metabolism, Animals, Cell Line, Ion Transport, Mice, Tetrahydroisoquinolines metabolism, Amides chemistry, Chlorides metabolism, Cystic Fibrosis Transmembrane Conductance Regulator metabolism, Tetrahydroisoquinolines chemistry
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 EC(50) values below 10nM in our cellular chloride transport assay.

Published
2005
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