SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs.

Leupyrrins are highly potent antifungal agents. A structure-activity-relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified leupylogs that incorporate a stable and readily available aromatic side chain. For their synthesis a concise strategy is described that enables a short and versatile access.