Abstract
Two scaffolds, one target: The bacterial ribosomal decoding site is the target for natural aminoglycoside antibiotics, which bind to an internal RNA loop and thereby interfere with translation fidelity. Synthetic aminoglycoside mimetics are thought to display similar antibiotic activity while avoiding established bacterial resistance mechanisms. We describe two complementary approaches towards novel aminoglycoside mimetics that recognize the decoding-site RNA and inhibit bacterial translation. In the first study, elements of both rational structure-based design and diversity-driven exploration were used to synthesize flexible acyclic mimetics (I a,b) of 2-deoxystreptamine. The second paper outlines the accurate replacement of the 2-deoxystreptamine pharmacophore by stereochemically defined aminomethyl–piperidine scaffolds (II a,b).
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: Chembiochem : a European journal of chemical biology
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
