Targeting bacterial cell division: A binding site-centered approach to the most promising inhibitors of the essential protein FtsZ

A Casiraghi, L Suigo, E Valoti, V Straniero - Antibiotics, 2020 - mdpi.com
Binary fission is the most common mode of bacterial cell division and is mediated by a
multiprotein complex denominated the divisome. The constriction of the Z-ring splits the …

1, 4-Benzodioxane, an evergreen, versatile scaffold in medicinal chemistry: A review of its recent applications in drug design

C Bolchi, F Bavo, R Appiani, G Roda… - European Journal of …, 2020 - Elsevier
Benzodioxane has long been a versatile template widely employed to design molecules
endowed with diverse bioactivities. Its use spans the last decades of medicinal chemistry …

Benzodioxane–Benzamides as FtsZ Inhibitors: Effects of Linker's Functionalization on gram-Positive Antimicrobial Activity

L Suigo, W Margolin, E Ulzurrun, M Hrast Rambaher… - Antibiotics, 2023 - mdpi.com
FtsZ is an essential bacterial protein abundantly studied as a novel and promising target for
antimicrobials. FtsZ is highly conserved among bacteria and mycobacteria, and it is crucial …

Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor

HK Lui, W Gao, KC Cheung, WB Jin, N Sun… - European journal of …, 2019 - Elsevier
The rapid emergence of methicillin-resistant Staphylococcus aureus (MRSA) strains has
undermined the therapeutic efficacy of existing β-lactam antibiotics (BLAs), prompting an …

Benzodioxane‐benzamides as antibacterial agents: computational and SAR studies to evaluate the influence of the 7‐substitution in FtsZ interaction

V Straniero, V Sebastián‐Pérez, M Hrast… - …, 2020 - Wiley Online Library
FtsZ is a crucial prokaryotic protein involved in bacterial cell replication. It recently arose as a
promising target in the search for antimicrobial agents able to fight antimicrobial resistance …

Computational design and development of benzodioxane-benzamides as potent inhibitors of FtsZ by exploring the hydrophobic subpocket

V Straniero, V Sebastián-Pérez, L Suigo, W Margolin… - Antibiotics, 2021 - mdpi.com
Multidrug resistant Staphylococcus aureus is a severe threat, responsible for most of the
nosocomial infections globally. This resistant strain is associated with a 64% increase in …

Antimicrobial action and reversal of resistance in MRSA by difluorobenzamide derivatives targeted at FtsZ

WC Chai, JJ Whittall, D Song, SW Polyak, AD Ogunniyi… - Antibiotics, 2020 - mdpi.com
The bacterial cell division protein, FtsZ, has been identified as a target for antimicrobial
development. Derivatives of 3-methoxybenzamide have shown promising activities as FtsZ …

Design, synthesis and biological evaluation of biphenyl-benzamides as potent FtsZ inhibitors

J Deng, T Zhang, B Li, M Xu, Y Wang - European Journal of Medicinal …, 2022 - Elsevier
The rapid emergence of antibiotic resistance has become a prevalent threat to public health,
thereby development of new antibacterial agents having novel mechanisms of action is in an …

T5S1607 identified as a antibacterial FtsZ inhibitor: Virtual screening combined with bioactivity evaluation for the drug discovery

Z Xie, W Ruan, J Guo, Y Li, S Zhou, J Zhao… - … Biology and Chemistry, 2024 - Elsevier
Due to antibiotic overuse, many bacteria have developed resistance, creating an urgent
need for novel antimicrobial agents. It has been established that the filamentous …

A mechanism of salt bridge–mediated resistance to FtsZ inhibitor PC190723 revealed by a cell-based screen

AK Sharma, SM Poddar, J Chakraborty… - Molecular biology of …, 2023 - Am Soc Cell Biol
Bacterial cell division proteins, especially the tubulin homologue FtsZ, have emerged as
strong targets for developing new antibiotics. Here, we have utilized the fission yeast …