296774-52-2Relevant academic research and scientific papers
A CHEMICALLY AND METABOLICALLY STABLE DIPEPTIDE POSSESSING POTENT SODIUM CHANNEL BLOCKER ACTIVITY
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Page/Page column 38; 39, (2013/03/26)
A very stable, selective and renally safe sodium channel blocker represented by the formula: The invention also includes a variety of compositions, combinations and methods of treatment usin this inventive sodium channel blocker.
Total synthesis and antifungal evaluation of cyclic aminohexapeptides
Klein, Larry L.,Li, Leping,Chen, Hui-Ju,Curty, Cynthia B.,Degoey, David A.,Grampovnik, David J.,Leone, Christina L.,Thomas, Sheela A.,Yeung, Clinton M.,Funk, Kenneth W.,Kishore, Vimal,Lundell, Edwin O.,Wodka, Dariusz,Meulbroek, Jon A.,Alder, Jeffrey D.,Nilius, Angela M.,Lartey, Paul A.,Plattner, Jacob J.
, p. 1677 - 1696 (2007/10/03)
The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of β-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the 'northwest' position imparts greatly improved water solubility (>5 mg/mL). The synthesis and structure-activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported. Copyright (C) 2000 Elsevier Science Ltd.
