Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann− Pick type C disease therapeutics

AI Rosenbaum, CC Cosner, CJ Mariani…

Index: Rosenbaum, Anton I.; Cosner, Casey C.; Mariani, Christopher J.; Maxfield, Frederick R.; Wiest, Olaf; Helquist, Paul Journal of Medicinal Chemistry, 2010 , vol. 53, # 14 p. 5281 - 5289

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Citation Number: 34

Abstract

Niemann− Pick type C (NPC) disease is a lysosomal storage disorder characterized at the cellular level by abnormal accumulation of cholesterol and other lipids in lysosomal storage organelles. Lysosomal acid lipase (LAL) has been recently identified as a potential therapeutic target for NPC. LAL can be specifically inhibited by a variety of 3, 4-disubstituted thiadiazole carbamates. An efficient synthesis of the C (3) oxygenated/C (4) aminated ...

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