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| - Conformationally Restricted (+)-Cacospongionolide B Analogues.Influence on Secretory Phospholipase A2 Inhibition
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| Abstract
| - A new approach to (+)-cacospongionolide was developed to access conformationally restricted variantsof the natural product. The flexible aliphatic region between the decalin and side chain portion of thenatural product was replaced with alkenyl and alkynyl linkers to probe the influence of structural rigidityin the inhibition of secretary phospholipase A2 (sPLA2). It was found that when the aliphatic section isreplaced with a Z-olefin or an alkyne, sPLA2 inhibitory activity suffered relative to the natural product;however, an E-olefin-containing analogue led to an enhanced activity. These results suggest that preferredsPLA2 binding conformation of the natural product is similar to the geometry of the E-olefin-containinganalogue.
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