Phospholipase A2 (PLA2) exists in extracellular (secretory) forms. Group II secretory PLA2 is an acute phase enzyme associated with several inflammatory diseases, so its inhibition may be useful for treating inflammatory and allergic diseases. In the course of searching for secretory PLA2 inhibitors from microorganisms, novel inhibitors WA8242A1, A2 and B were obtained from the cultured mycelium of Streptomyces violaceusniger No. 8242. These compounds are structurally related with α-aminoadipic acid and various length of alkyl chains, and show stronger inhibitory activity against group II PLA2 than against group I PLA2. This paper describes the taxonomy of the producing strain, production and purification of these inhibitors. Biological properties are described in an accompanying paper, and structure elucidation and total synthesis will be published subsequently.