Fighting antibiotic resistance—strategies and (pre) clinical developments to find new antibacterials

S Walesch, J Birkelbach, G Jézéquel, FPJ Haeckl… - EMBO …, 2023 - embopress.org
Antibacterial resistance is one of the greatest threats to human health. The development of
new therapeutics against bacterial pathogens has slowed drastically since the approvals of …

Fluoroquinolones hybrid molecules as promising antibacterial agents in the fight against antibacterial resistance

IA Lungu, OL Moldovan, V Biriș, A Rusu - Pharmaceutics, 2022 - mdpi.com
The emergence of bacterial resistance has motivated researchers to discover new
antibacterial agents. Nowadays, fluoroquinolones keep their status as one of the essential …

Novel formats of antibody conjugates: recent advances in payload diversity, conjugation, and linker chemistry

T Fujii, Y Matsuda - Expert Opinion on Biological Therapy, 2023 - Taylor & Francis
Introduction In the field of bioconjugates, the focus on antibody–drug conjugates (ADCs)
with novel payloads beyond the traditional categories of potent cytotoxic agents is …

Beyond the approved: target sites and inhibitors of bacterial RNA polymerase from bacteria and fungi

SH Kirsch, FPJ Haeckl, R Müller - Natural Product Reports, 2022 - pubs.rsc.org
Covering: 2016 to 2022 RNA polymerase (RNAP) is the central enzyme in bacterial gene
expression representing an attractive and validated target for antibiotics. Two well-known …

Design, synthesis, and characterization of TNP-2198, a dual-targeted rifamycin-nitroimidazole conjugate with potent activity against microaerophilic and anaerobic …

Z Ma, S He, Y Yuan, Z Zhuang, Y Liu… - Journal of medicinal …, 2022 - ACS Publications
TNP-2198, a stable conjugate of a rifamycin pharmacophore and a nitroimidazole
pharmacophore, has been designed, synthesized, and evaluated as a novel dual-targeted …

Multitarget antibacterial drugs: An effective strategy to combat bacterial resistance

J Feng, Y Zheng, W Ma, A Ihsan, H Hao… - Pharmacology & …, 2023 - Elsevier
The rise of antibiotic resistance and the decrease in the discovery of new antibiotics have
caused a global health crisis. Of particular concern is the fact that despite efforts to develop …

Safety, pharmacokinetics, and efficacy of rifasutenizol, a novel dual-targeted antibacterial agent in healthy participants and patients in China with Helicobacter pylori …

X Li, Y Liu, M Wang, L Gao, J Liu, H Zhang… - The Lancet Infectious …, 2024 - thelancet.com
Background Due to the rapid development of antimicrobial resistance, the efficacy of most
Helicobacter pylori eradication therapies have progressively decreased to an unacceptable …

Towards Antibacterial Agents: Synthesis and Biological Activity of Multivalent Amide Derivatives of Thiacalix [4] Arene with Hydroxyl and Amine Groups

I Shiabiev, D Pysin, A Akhmedov, O Babaeva… - Pharmaceutics, 2023 - mdpi.com
Antimicrobial resistance to modern antibiotics stimulates the search for new ways to
synthesize and modify antimicrobial drugs. The development of synthetic approaches that …

An update review of approaches to multiple action-based antibacterials

JB Bremner - Antibiotics, 2023 - mdpi.com
Many approaches are being pursued to address the major global health challenge posed by
the increasing resistance of pathogenic bacteria to antibacterial agents. One of the …

Antistaphylococcal discovery pipeline; where are we now?

D Nawrot, W Ambrożkiewicz-Mosler, M Doležal… - European Journal of …, 2023 - Elsevier
The serious spread of antibiotic-resistant staphylococcal aureus strains is alarming. This is
reflected by the measures governments and health related bodies are offering to ease …