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