Polyheterocyclic peptidomimetics: Parallel solid phase synthesis of oligo cyclic guanidines and their inhibition activity against Mycobacterium tuberculosis DNA gyrase

Polyheterocycles are one of the most desired synthetic targets due to their numerous and valuable applications in various fields. We report the design and the parallel synthesis of novel linear oligocyclic guanidine peptidomimetics from predesigned reduced polyamides. A screening of these compounds identified active Mycobacterium tuberculosis DNA gyrase inhibitors which do not inhibit human DNA topoisomerase II & alpha; and topoisomerase I.

Automated summary

Polyheterocycles are desirable synthetic targets with valuable applications. This study reports the parallel synthesis of novel linear oligocyclic guanidine peptidomimetics and their screening as Mycobacterium tuberculosis DNA gyrase inhibitors. These compounds do not inhibit human DNA topoisomerase IIα and topoisomerase I.