Abstract: It is summarized that biologically active pyrroles and their structurally related compounds are naturally occurring from plants, insects and microorganisms. Synthetic arylpyrrole pesticides, such as chlorfenapyr, have been discovered and developed through chemical modification of pyrrole antibiotics. The synthetic arylpyrrole compounds, with a characteristic of structural diversity and broad spectrum of biological activities, have been paid more attention for past decade and are still in progress.