Structure-activity relationship and design of an antimutagen against the UV-induced mutation of Escherichia coli.

Abstract

Structure-activity relationships of antimutagens were studied by assaying analogues and derivatives of 2(5H)furanone designed on the basis of the structures of natual antimutagens by the method of observing UV-induced reversion of E. coli WP2 B/r uvr A- trp E-. It is shown that an α, β-unsaturated carbonyl system is required for antimutagenic activity. Further modification of 3(2H)furanones resulted in the development of a highly potent antimutagen. The possibility that the antimutagenic effects may be due to alteration of proteins involved in the DNA repair system by trapping thiol groups is also discussed.