862506-77-2Relevant academic research and scientific papers
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport
Hirth, Bradford H.,Qiao, Shuang,Cuff, Lisa M.,Cochran, Brian M.,Pregel, Marko J.,Gregory, Jill S.,Sneddon, Scott F.,Kane Jr., John L.
, p. 2087 - 2091 (2007/10/03)
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.
Tetrahydroisoquinoline derivatives for treating protein trafficking diseases
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Page/Page column 11, (2008/06/13)
Tetrhydroisoquinoline derivatives, pharmaceutical compositions comprising them and methods of treating disease are disclosed herein. The disclosed compounds are useful in the treatment and prevention of diseases mediated by chloride channel activity and/or protein trafficking, including, but not limited to, diseases associated with impaired mucociliary clearance such as cystic fibrosis, bronchitis, emphysema, and the like.
