SYNTHESIS AND BIOLOGICAL-ACTIVITY OF ALLOSAMIDIN AND ALLOSAMIDIN ANALOGS

The chitinase inhibitor/insect ecdysis inhibitor allosamidin and eight allosamidin analogues have been synthesised from simple carbohydrate starting materials. Allosamidin was assayed against Tineola bisselliel la (Hummel) larvae and all nine compounds were examined for their effe cts on the development of larvae of Lucilia cuprina (Wiedemann). High larval mortality compared to controls resulted when T. bisselliella an d L. cuprina larva were exposed to allosamidin. The (1 --> 3) linked r egioisomer, the dimeric analogue and the gluco-configurated dimeric an alogue of allosamidin all showed high activity against L. cuprina larv ae. The regioisomer, the (1 --> 3) linked isomer and its dimeric analo gue, as well as the monomer allosamizoline and its regioisomer, were i nactive, These new in-vivo results are consistent with known in-vitro insect chitinase inhibition data, in that greatest larval mortality wa s exhibited by the best inhibitors.