Zwitterionic sulfobetaine inhibitors of squalene synthase

…, DE Blanchard, A Castro, P Gu, G Jiang…

Index: Spencer, Thomas A.; Onofrey, Thomas J.; Cann, Reginald O.; Russel, Jonathon S.; Lee, Laura E.; Blanchard, Daniel E.; Castro, Alfredo; Gu, Peide; Jiang, Guojian; Shechter, Ishaiahu Journal of Organic Chemistry, 1999 , vol. 64, # 3 p. 807 - 818

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Citation Number: 49

Abstract

A substantial number of sulfobetaines (eg, 10) have been synthesized and evaluated as inhibitors of squalene synthase (SS) on the basis of the idea that their zwitterionic structure would have properties conducive both to binding in the active site and to passage through cell membranes. When the simple sulfobetaine moiety is incorporated into compounds containing hydrophobic portions like those in farnesyl diphosphate (1) or presqualene ...