Multitargeting compounds: a promising strategy to overcome multi-drug resistant tuberculosis

G Stelitano, JC Sammartino, LR Chiarelli - Molecules, 2020 - mdpi.com
Tuberculosis is still an urgent global health problem, mainly due to the spread of multi-drug
resistant M. tuberculosis strains, which lead to the need of new more efficient drugs. A …

Mechanochemical synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity

PFM Oliveira, B Guidetti, A Chamayou, C André-Barrès… - Molecules, 2017 - mdpi.com
A series of isoniazid derivatives bearing a phenolic or heteroaromatic coupled frame were
obtained by mechanochemical means. Their pH stability and their structural …

Mycobacterial fatty acid catabolism is repressed by FdmR to sustain lipogenesis and virulence

W Dong, X Nie, H Zhu, Q Liu, K Shi… - Proceedings of the …, 2021 - National Acad Sciences
Host-derived fatty acids are an important carbon source for pathogenic mycobacteria during
infection. How mycobacterial cells regulate the catabolism of fatty acids to serve the …

Insights into Acinetobacter baumannii fatty acid synthesis 3-oxoacyl-ACP reductases

EM Cross, FG Adams, JK Waters, D Aragão… - Scientific reports, 2021 - nature.com
Treatments for 'superbug'infections are the focus for innovative research, as drug resistance
threatens human health and medical practices globally. In particular, Acinetobacter …

Synthesis, antimicrobial capability and molecular docking of heterocyclic scaffolds clubbed by 2-azetidinone, thiazole and quinoline derivatives

NC Desai, JP Harsora, JD Monapara… - Polycyclic Aromatic …, 2022 - Taylor & Francis
A new set of molecules was designed and synthesized by compilation of pharmacologically
potential segments thiazole and quinoline bridged by 2-azetidinone as a linker in a single …

2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents

R Geesala, JK Gangasani, M Budde… - European journal of …, 2016 - Elsevier
A series of twenty-five 2-azitidinone (β-lactam) derivatives were synthesized and evaluated
for anti-cancer properties against breast cancer, MCF-7 and MDA-MB-231. These β-lactam …

Harnessing polypharmacology with computer-aided drug design and systems biology

H Wathieu, NT Issa, SW Byers… - Current …, 2016 - ingentaconnect.com
The ascent of polypharmacology in drug development has many implications for disease
therapy, most notably in the efforts of drug discovery, drug repositioning, precision medicine …

Synthesis of 1, 3-diaryl-spiro [azetidine-2, 3′-indoline]-2′, 4-diones via the Staudinger reaction: cis-or trans-diastereoselectivity with different addition modes

V Filatov, M Kukushkin, J Kuznetsova, D Skvortsov… - RSC …, 2020 - pubs.rsc.org
A new synthetic approach for realizing biologically relevant bis-aryl spiro [azetidine-2, 3′-
indoline]-2′, 4-diones was developed based on Staudinger ketene–imine cycloaddition …

Structural and functional characterization of FabG4 from Mycolicibacterium smegmatis

X Ran, P Parikh, J Abendroth, TL Arakaki… - … Section F: Structural …, 2024 - journals.iucr.org
The rise in antimicrobial resistance is a global health crisis and necessitates the
development of novel strategies to treat infections. For example, in 2022 tuberculosis (TB) …

Access to 2-oxoazetidine-3-carboxylic acid derivatives via thermal microwave-assisted Wolff rearrangement of 3-diazotetramic acids in the presence of nucleophiles

I Lyutin, V Krivovicheva, G Kantin… - Beilstein Journal of …, 2024 - beilstein-journals.org
In this work, we report an efficient approach to 2-oxoazetidine-3-carboxylic acid derivatives
based on a thermally promoted Wolff rearrangement of diazotetramic acids in the presence …