SULFOBETAINE ZWITTERIONIC INHIBITORS OF SQUALENE SYNTHASE

Citation
I. Shechter et al., SULFOBETAINE ZWITTERIONIC INHIBITORS OF SQUALENE SYNTHASE, Bioorganic & medicinal chemistry letters, 6(21), 1996, pp. 2585-2588
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
6
Issue
21
Year of publication
1996
Pages
2585 - 2588
Database
ISI
SICI code
0960-894X(1996)6:21<2585:SZIOSS>2.0.ZU;2-O
Abstract
Zwitterions such as farnesyl sulfobetaine 8 are a new type of inhibito r of squalene synthase that, while maintaining overall neutrality, mim ic both the carbocationic and anionic moieties of presumed reaction in termediates. The most effective zwitterionic sulfobetaines discovered to date are aromatic derivatives 17 (IC50 = 2 mu M) and 20 (IC50 = 5 m u M). Copyright (C) 1996 Elsevier Science Ltd