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Inhibitors of Bacterial DNA Synthesis

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Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...

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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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Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to cholesterol contributes to...

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Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...

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Related Experiment Video

Updated: May 30, 2026

Assay Development for High-Throughput Drug Screening Against Mycobacteria

Assay Development for High-Throughput Drug Screening Against Mycobacteria

Published on: October 25, 2024

Fidaxomicin: first-in-class macrocyclic antibiotic.

Kathleen M Mullane¹, Sherwood Gorbach

¹Department of Medicine, University of Chicago, Chicago, IL, USA. kmullane@medicine.bsd.uchicago.edu

Expert Review of Anti-Infective Therapy

|August 4, 2011

Summary

Clostridium difficile infection (CDI) is a growing concern. Fidaxomicin shows superior cure rates compared to vancomycin for treating CDI, offering a promising new option for this serious infection.

Area of Science:

Infectious Diseases
Microbiology
Pharmacology

Background:

Clostridium difficile infection (CDI) incidence has doubled in 15 years, leading to increased mortality.
CDI is now the leading cause of nosocomial infections, surpassing MRSA.
Current CDI therapies have insufficient response rates, necessitating novel treatments.

Purpose of the Study:

To evaluate fidaxomicin as a novel treatment for Clostridium difficile infection.
To compare the efficacy of fidaxomicin against vancomycin in CDI treatment.
To assess the global cure rate, including recurrence, for fidaxomicin therapy.

Main Methods:

Two robust clinical trials were conducted.
Fidaxomicin was compared directly to vancomycin for CDI treatment.

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A Protocol to Characterize the Morphological Changes of Clostridium difficile in Response to Antibiotic Treatment

A Protocol to Characterize the Morphological Changes of Clostridium difficile in Response to Antibiotic Treatment

Published on: May 25, 2017

Global cure rates (cure without recurrence) were analyzed.

Main Results:

Fidaxomicin demonstrated a superior global cure rate compared to vancomycin.
This outcome was observed in two independent clinical trials.
Fidaxomicin represents a new class of macrocyclic antimicrobial agents.

Conclusions:

Fidaxomicin offers an advance in the management of Clostridium difficile infection.
Its superior efficacy over vancomycin suggests a new standard of care.
Further research into novel antimicrobial agents for CDI is warranted.