Review article

https://doi.org/10.5562/cca4325

Macrolide Structure, Bioactivity and Interactions: a Review

Ivana Mikulandra ; TAPI Croatia Industries Ltd., Prudnička cesta 54, Prigorje Brdovečko
Iva Habinovec ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, 10000 Zagreb, Croatia
Tomislav Jednačak ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, 10000 Zagreb, Croatia
Predrag Novak ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, 10000 Zagreb, Croatia *

* Corresponding author.

Abstract

Since the discovery of macrolide antibiotics, extensive research has been focused on the development of new bioactive compounds in response to an emerging number of multidrug-resistant pathogens. In the last several decades, macrolide antibiotics have made a significant contribution to human healthcare. Nevertheless, interest in the development of broad-spectrum macrolides remains due to increasing bacterial resistance. This review summarizes recent advances in macrolide synthesis and discusses alternative strategies for structural modification of macrolides, highlighting how these modifications affect their bioactivity through structure-activity relationship (SAR) and interaction studies. It provides an insight into the macrolide binding mechanisms to their biomolecular targets that play key roles in the overall biological profile of a drug. Recently reported structures of macrolide complexes with biomolecules have also been summarized, providing a platform for the design of new antibiotics active against resistant bacteria.

Keywords

macrolides; bacterial resistance; structure and bioactivity; biomolecular targets and interactions

Hrčak ID:

347425

URI

https://hrcak.srce.hr/347425

Publication date:

21.5.2026.

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