Biologically-active indole-containing compound-natural products from sponges and their synthetic analogs

Abstract

Guided by the inhibitory activities of indole-containing marine natural products against isocitrate lyase (ICL) from Candida albicans and sortase A (SrtA) from Staphylococcus aureus, a series of compounds structurally analogous to natural products were synthesized. Eight Srt A inhibitors and two ICL inhibitors having higher activities than the natural products were discovered by screening the enzyme inhibitory activities of synthesized compounds. Among the Srt A inhibitors discovered, six exhibited higher activities than p-hydroxymercuribenzoic acid, which suggests that these compounds have great potential as alternative antibacterial agents.roducts were synthesized. Eight Srt A inhibitors and two ICL inhibitors having higher activities than the natural products were discovered by screening the enzyme inhibitory activities of synthesized compounds. Among the Srt A inhibitors discovered, six exhibited higher activities than p-hydroxymercuribenzoic acid, which suggests that these compounds have great potential as alternative antibacterial agents.