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Inhibitors of Bacterial Protein Synthesis

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Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...

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Updated: Jun 10, 2026

Antibiotic Dereplication Using the Antibiotic Resistance Platform

Antibiotic Dereplication Using the Antibiotic Resistance Platform

Published on: October 17, 2019

New aminoglycoside antibiotics.

Paola Dozzo¹, Heinz E Moser

¹Achaogen, Inc., 7000 Shoreline Court, South San Francisco, CA 94080, USA.

Expert Opinion on Therapeutic Patents

|July 31, 2010

Summary

The dormant field of aminoglycoside (AG) antibiotics is reawakening with novel chemical modifications targeting multi-drug resistant Gram-negative bacteria. One promising clinical candidate, ACHN-490, is advancing in trials for urinary tract infections.

Area of Science:

Pharmaceutical Chemistry
Infectious Diseases
Drug Discovery

Background:

Rising incidence of nosocomial infections caused by multi-drug resistant (MDR) Gram-negative bacteria.
Limited therapeutic options for MDR Gram-negative bacterial infections.
Aminoglycosides (AGs) are a key antibiotic class with activity against Gram-negative bacteria.

Purpose of the Study:

To review the patent literature on novel aminoglycoside analogs.
To assess the therapeutic potential of these derivatives against MDR Gram-negative pathogens.
To identify recent advancements in aminoglycoside antibiotic development.

Main Methods:

Comprehensive summary of aminoglycoside patent literature from 2005 to 2010.
Focus on novel AG analogs with potential against MDR Gram-negative pathogens.

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Assessment of therapeutic potential for described AG derivatives.

Main Results:

Overview of patent activity in the AG field over the last five years.
Identification of novel AG derivatives with potential therapeutic applications.
Evaluation of the therapeutic promise of these new compounds.

Conclusions:

Recent resurgence in AG antibiotic research by academic and industrial groups.
Application of novel technologies in developing new AGs.
One clinical candidate, ACHN-490, is in Phase II trials for complicated urinary tract infections.