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

Bioorg Med Chem Lett

Center for Translational Science, Florida International University, 11350 SW Village Parkway, Port Saint Lucie, FL 34987, USA; Herbert Wertheim College of Medicine, FIU, 11200 SW 8th St, Miami, FL 33199, USA. Electronic address:

Published: September 2023

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 IIα and topoisomerase I.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10993493PMC
http://dx.doi.org/10.1016/j.bmcl.2023.129439DOI Listing

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