Synthesis and evaluation of new marinoquinolines with potential antimalarial activity

Marinoquinoline A was isolated from the gliding bacterium Ohtaekwangia kribbensis together with the novel marinoquinolines B-F (Figure 1). [1,2,3] These compounds have demonstrated moderate antiprotozoal activity against Plasmodium falciparum K1 (chloroquine resistant, IC50 1.7 to 15 µM) and Trypanosoma cruzi (IC50 21.8 to 53.1 µM).

Figure 1. Structures of the natural marinoquinolines

Thus, bearing in mind the pharmacological potential of marinoquinolines, the present work describes the synthesis of novel marinoquinoline derivatives as promising potential compounds as new chemical entities against P. falciparum. Pyrroloanilines intermediates were synthesized by Suzuki-Miyuara reactions followed by Pictet-Spengler reactions to obtain the desired marinoquinolines in good overall yields (scheme).
The new marinoquinolines were evaluated for their antimalarial activities and have showed good antimalarial activity