One-pot synthesis and biological evaluation of aspergillamides and analogues

A one-pot total synthesis of aspergillamide and analogues by a solution phase Ugi multi component reaction (MCR) is described. The reaction is easily performed in 96-well plates and offers a facile access to diverse aspergillamide analogue compound libraries. The antibiotic and cytotoxic activity of these compounds is measured. Several of them are more potent than the natural product. (C) 2000 Elsevier Science Ltd. All rights reserved.