Abstract

The tetracycline antibiotic class has acquired new valuable members due to the optimisation of the chemical structure. The first modern tetracycline introduced into therapy was tigecycline, followed by omadacycline, eravacycline, and sarecycline (the third generation). Structural and physicochemical key elements which led to the discovery of modern tetracyclines are approached. Thus, several chemical subgroups are distinguished, such as glycylcyclines, aminomethylcyclines, and fluorocyclines, which have excellent development potential. The antibacterial spectrum comprises several resistant bacteria, including those resistant to old tetracyclines. Sarecycline, a narrow-spectrum tetracycline, is notable for being very effective against Cutinebacterium acnes. The mechanism of antibacterial action from the perspective of the new compound is approached. Several severe bacterial infections are treated with tigecycline, omadacycline, and eravacycline (with parenteral or oral formulations). In addition, sarecycline is very useful in treating acne vulgaris. Tetracyclines also have other non-antibiotic properties that require in-depth studies, such as the anti-inflammatory effect effect of sarecycline. The main side effects of modern tetracyclines are described in accordance with published clinical studies. Undoubtedly, this class of antibiotics continues to arouse the interest of researchers. As a result, new derivatives are developed and studied primarily for the antibiotic effect and other biological effects.

Highlights

  • Received: 29 October 2021Accepted: 3 December 2021Published: 5 December 2021Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.Tetracyclines are an important class of broad-spectrum antibiotics that prevent bacterial growth by inhibiting protein biosynthesis

  • The penetration of aminoacyl transporter RNA into the acceptor site (A) on the bacterial ribosome is blocked, the consequence being the cessation in the incorporation of amino acids residues in the process of elongation of the polypeptide chain

  • On the basis of the classical method of production, biosynthesis, and semi-synthesis, we are able to obtain the new compounds by total chemical synthesis, such as eravacycline

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Summary

Introduction

Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Tetracyclines are an important class of broad-spectrum antibiotics that prevent bacterial growth by inhibiting protein biosynthesis. This large family includes compounds with bacteriostatic activity and a wide range of uses, from Gram-positive and Gram-negative bacterial infections to those caused by a protozoan parasite and intracellular organisms [1]. Sarecycline is unique, being the only narrow-spectrum antibiotic in the tetracycline-class family. The basic structure of tetracyclines consists of four linearly condensed benzene rings in a hydronaphtacene nucleus. The essential differences between the analogues of this class are given by the C5, C6, C7, and C9 substituents (Figure 1) [2]

Brief History of Tetracycline Antibiotics
Obtaining Method
Considerations Regarding the Chemical Structure and Physicochemical Properties of the
C N NC HC3H 3
Structure-Activity Relationships
Mechanism of Action
Spectrum of Antibacterial Activity
Bacterial Resistance to New Tetracyclines
Therapeutic Use of the New Tetracyclines
Side Effects of the Third-Generation Tetracyclines
New Compounds under Development
13. Promising
Findings
Conclusions
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