Synthetic Analogues of Naturally Occurring Spider Toxins

Naturally occurring spider toxins are potent inhibitors of glutamate receptors of the central nervous system and have the general structure (hetero)arylacyl→aminoacyl( I )→polyamine→aminoacyl( II ) (the arrow indicates the direction of an amide linkage). In the present paper, the synthesis of the ten spider-toxin analogues 13 , 18 , 21 , 28 , 35 , 37 , 39 , 41 , 45 , and 53 are reported (Schemes 1–12). These compounds differ in their subunits and, in some cases, in the sequence of these moieties.