1 research outputs found
Extensive structureâactivity relationship study of albicidinâs Câterminal dipeptidic pâaminobenzoic acid moiety
Albicidin is a recently described natural product that strongly inhibits bacterial DNA gyrase. The pronounced activity, particularly against Gramânegative bacteria, turns it into a promising lead structure for an antibacterial drug. Hence, structureâactivity relationship studies are key for the inâdepth understanding of structural features/moieties affecting gyrase inhibition, antibacterial activity and overcoming resistance. The 27â
newly synthesized albicidins give profound insights into possibilities for variations of the Câterminus. Furthermore, in the present study, a novel derivative has been identified as overcoming resistance posed by the Klebsiellaâprotease AlbD. Structural modifications include, for example, azahistidine replacing the previous instable cyanoalanine as the central amino acid, as well as a triazole amide bond isostere between building blocksâ
D and E.BMBF, 03VP00030, Validierung einer neuen antibakteriellen Wirkstoffklasse - AlbiPharmTU Berlin, Open-Access-Mittel - 201