Date of Award
2013
Document Type
Thesis
Publication Status
Version of Record
Submission Date
October 2026
Abstract
With antimicrobial resistance to current drugs steadily rising, the development of new antibiotics with novel mechanisms of action has become an imperative. The majority of life-threatening infections worldwide are caused by "ESKAPE" pathogens which are encountered in more than 40% of hospital-acquired infections, and are resistant to the majority of commonly used antibiotics. Naturally occurring cyclic depsipeptides, microbial secondary metabolites that contain one or more ester bonds in addition to amide bonds, have emerged as an important source of pharmacologically active compounds or lead structures for the development of novel antibiotics. Some of those peptides are either already marketed (daptomycin) or in advanced stages of clinical development (ramoplanin). Structurally simple, yet potent, fusaricidin/LI-F and lysobactin families of naturally occurring antibiotics represent particularly attractive candidates for the development of new antibacterial agents capable of overco ming infections caused by multidrug-resistant bacteria. These natural products exhibit potent antimicrobial activity against a variety of clinically relevant fungi and Gram-positive bacteria. Therefore, access to these classes of natural products and their synthetic analogs, combined with elucidation of their mode of action represent important initial steps toward full exploitation of their antmicrobial potential. This dissertation describes a general approach toward the solid-phase synthesis of fusaricidin/LI-F and lysobactin analogs and an extensive structure-activity relationship (SAR) study. We have devised a simple and robust preparation strategy based on standard Fmoc solid-phase peptide synthesis protocols.
Extent
xv, 197 p. : ill. (some col.)
Recommended Citation
Bionda, Nina., "Cyclic lipodepsipeptides as lead structures for the discovery of new antiobiotics" (2013). Electronic Theses and Dissertations 2010 - 2019. 729.
https://digitalcommons.fau.edu/etd_general_6/729
Identifier
FADT3360768
Comments
by Nina Bionda.|Thesis (Ph.D.)--Florida Atlantic University, 2013.|Includes bibliography.|Mode of access: World Wide Web.|System requirements: Adobe Reader.|by Nina Bionda.