From Natural Product‐Inspired Pyrrolidine Scaffolds to the Development of New Human Golgi α‐Mannosidase II Inhibitors

Abstract

A little inspiration: The systematic preparation of sixteen natural product-inspired polyhydroylated pyrrolidine-based isomeric scaffolds is described. Each scaffold possesses four stereogenic centers and one exo-aminomethyl moiety, which allows for rapid substituent diversity. To exemplify biological applications, these new privileged scaffolds were used to discover new human Golgi α-mannosidase II inhibitors. The most potent inhibitor shows competitive behavior with a Ki value of 24 nM. As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.