78573-84-9Relevant academic research and scientific papers
Zwitterionic sulfobetaine inhibitors of squalene synthase
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
, p. 807 - 818 (2007/10/03)
A substantial number of sulfobetaines (e.g., 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 diphosphate (2), inhibition of SS in a rat liver microsomal assay was indeed observed. For example, farnesylated sulfobetaine 10 has IC50 = 10 μM and aromatic derivative 35 has IC50 = 2 μM for SS inhibition. A wide variety of structural modifications, exemplified by compounds 43, 52, 76, 85, 91, 99, 111, and 115, was investigated. Unfortunately, no inhibitors in the submicromolar range were discovered, and exploration of a different type of zwitterion seems necessary if this appealing approach to inhibition of SS is going to provide a potential antihypercholesterolemic agent.
Substituted oxiranecarboxylic acids, their use and medicaments containing them
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, (2008/06/13)
Substituted oxiranecarboxylic acids of the formula STR1 wherein R1 denotes a hydrogen atom (--H), a halogen atom, a hydroxylroup, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R2 has one of the meanings of Rs
