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Updated: Mar 10, 2026
Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection
Published on: October 25, 2013
Novel Antibacterial Compounds and their Drug Targets - Successes and Challenges
Agnieszka A Kaczor1, Andrzej Polski2, Karolina Sobótka-Polska3
1Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modeling Lab, Faculty of Pharmacy with Division of Medical Analytics, Medical University of Lublin, 4A Chodzki St., PL-20093 Lublin. Poland.
Abstract:
Infectious diseases are one of the most important and urgent health problems in the world. According to the World Health Organization (WHO) statistics, infectious and parasitic diseases are a cause of about 16% of all deaths worldwide and over 40% of deaths in Africa. A considerable progress that has been made during last hundred years in the fight against infectious diseases, in particular bacterial infections, can be attributed mainly to three factors: (1) the general improvement of living conditions, in particular sanitation; (2) development of vaccines and (3) development of efficient antibacterial drugs. Although considerable progress in reduction of the number of cases of bacterial infections, especially in lethal cases, has been made, continued cases and outbreaks of these diseases persist, which is caused by different contributing factors. Indeed, during last sixty years antibacterial drugs were used against various infectious diseases caused by bacterial pathogens with an undoubtable success. The most fruitful period for antibiotic development lasted from 40's to 60's of the last century and resulted in the majority of antibiotics currently on the market, which were obtained by screening actinomycetes derived from soil. Although the market for antibacterial drugs is nowadays greater than 25 billion US dollars per year, novel antibacterial drugs are still demanded due to developed resistance of many pathogenic bacteria against current antibiotics. In the last five years, one can observe a dramatic increase in cases of resistant bacteria strains (e.g. Klebsiella pneumoniae and E. coli) which are responsible for difficult to treat pneumonia and infections of urinary tract. The development of resistant bacteria strains is a side effect of antibiotic application for treatment: the infections become untreatable as a result of the existence of antibiotic-tolerant persisters. In this review, we discuss the challenges in antibacterial drug discovery, including the molecular basis of drug resistance, drug targets for novel antibacterial drugs, and new compounds (since year 2010) from different chemical classes with antibacterial activity, focusing on structure-activity relationships.
Insights
Antibiotic resistance is a growing global health crisis, with increasing cases of untreatable bacterial infections. This review explores challenges and new discoveries in antibacterial drug discovery to combat resistant pathogens.
Area of Science:
- Microbiology
- Pharmacology
- Infectious Diseases
Background:
- Infectious diseases remain a critical global health concern, causing significant mortality worldwide, particularly in Africa.
- While advancements in sanitation, vaccines, and antibacterial drugs have reduced infectious disease deaths, persistent outbreaks and resistance pose ongoing challenges.
- The discovery of antibiotics, primarily from soil-derived actinomycetes between the 1940s and 1960s, revolutionized bacterial infection treatment, creating a multi-billion dollar market.
Purpose of the Study:
- To review the challenges in antibacterial drug discovery.
- To examine the molecular basis of antibiotic resistance and identify potential drug targets.
- To highlight novel antibacterial compounds discovered since 2010, analyzing their structure-activity relationships.
Main Methods:
- Literature review of infectious disease statistics and antibiotic development history.
- Analysis of the mechanisms underlying bacterial resistance to current antibiotics.
- Survey of recent (post-2010) antibacterial drug candidates and their chemical properties.
Main Results:
- A significant increase in antibiotic-resistant bacteria, such as Klebsiella pneumoniae and E. coli, has been observed, leading to difficult-to-treat infections.
- Antibiotic tolerance in 'persister' cells contributes to the development of untreatable infections.
- Recent research has identified new chemical classes of compounds with antibacterial activity.
Conclusions:
- Novel antibacterial drug discovery is urgently needed to address the escalating threat of antimicrobial resistance.
- Understanding resistance mechanisms and identifying new drug targets are crucial for developing effective treatments.
- Continued research into novel compounds and their structure-activity relationships is essential for future antibacterial therapies.
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