Design, Synthesis, and Structure–Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors

Abstract excerpt

ZAK is a new promising target for discovery of drugs with activity against antihypertrophic cardiomyopathy (HCM). A series of 1,2,3-triazole benzenesulfonamides were designed and synthesized as selective ZAK inhibitors. One of these compounds, 6p binds tightly to ZAK protein ( K d = 8.0 nM) and potently suppresses the kinase function of ZAK with single-digit nM (IC 50 = 4.0 nM) and exhibits excellent selectivity...

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