New furin inhibitors based on weakly basic amidinohydrazones

基于弱碱性脒基腙的新型弗林蛋白酶抑制剂

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Abstract

A novel series of amidinohydrazone-derived furin inhibitors was prepared; the most potent compounds 17 and 21 inhibit furin with K(i) values of 0.46 and 0.59μM, respectively. In contrast to inhibitor 17, which still contains a guanidino residue, compound 21 possesses only weakly basic amidinohydrazone groups.

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