Structural Optimization of Antimycobacterial Azaaurones Towards Improved Solubility and Metabolic Stability

A Campaniço, SG Harjivan, E Freitas… - …, 2023 - Wiley Online Library
… drug resistant TB (pre-XDRTB) and extensively drug-resistant TB (XDR-TB), rare types of
MDR-TB … with and without albumin, validating azaaurones as potent antimycobacterial agents. …

[HTML][HTML] Synthesis and anticancer cytotoxicity of azaaurones overcoming multidrug resistance

S Tóth, Á Szepesi, VK Tran-Nguyen, B Sarkadi… - Molecules, 2020 - mdpi.com
… the existence of compounds with potent in vitro activity [2]. … cytotoxic agents, we decided
to focus on azaaurones where … the design of leishmanicidal and antibacterial agents [23,24,…

Hit optimization to improve aqueous solubility of compounds with antimycobacterial activity

ECS Freitas - 2020 - repositorio.ul.pt
… group discovered that azaaurone based scaffold displays optimal antimycobacterial activity,
… Moreover, 6.2% of MDR-TB cases represent extensively-resistant TB (XDRTB) that include …

[HTML][HTML] Identification of anti-tuberculosis compounds from aurone analogs

D Yang, ZE Taylor, S Handy, S Li, J Liu… - Frontiers in …, 2020 - frontiersin.org
TB drugs. Simpler drug regimens that are safe, well tolerated, and effective against MDR/XDR
TB … We selected two azaaurone leads and two aurone leads that had high SIs on the three …

Design, synthesis and characterization of functionalized pyrazole derivatives bearing amide and sulfonamide moieties from aza-aurones

M Chalkha, M Bakhouch, M Akhazzane… - Journal of Chemical …, 2020 - Springer
aza-aurones. Firstly, the intermediate spiropyrazolines were obtained through a highly
regioselective 1,3-dipolar cycloaddition of nitrilimines with aza-aurones. … Aza-aurones 1 was used …

… response, disease progression, and medicinal chemistry efforts in the last decade toward the development of potential drugs for extensively drug-resistant …

A Sharma, M De Rosa, N Singla, G Singh… - Journal of medicinal …, 2021 - ACS Publications
… resistance to strong first-line anti-TB drugs (isoniazid and … for the treatment of drug-resistant
TB, seem to have become … The mechanism of action of azaaurones still remains unclear…

[HTML][HTML] Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs

M Eymery, VK Tran-Nguyen, A Boumendjel - Pharmaceuticals, 2021 - mdpi.com
… In this context, azaaurones were investigated as anticancer agents [72] and antibacterial
and … Interestingly, azocanes were also reported as potent dual NK1 receptor antagonist-…

[HTML][HTML] Scaffold-Hopping Strategies in Aurone Optimization: A Comprehensive Review of Synthetic Procedures and Biological Activities of Nitrogen and Sulfur …

G La Monica, F Alamia, A Bono, A Lauria, A Martorana - Molecules, 2024 - mdpi.com
… , high kinetic solubility, and improved antimycobacterial activity (in the sub-micromolar range…
to azaaurone appeared to be suitable for developing compounds with potent antiviral activity

Bioactive aurones, indanones, and other hemiindigoid scaffolds: medicinal chemistry and photopharmacology perspectives

LM Lazinski, G Royal, M Robin… - Journal of Medicinal …, 2022 - ACS Publications
… and hemithioindigos (sometimes azaaurones and thioaurones, … indanone derivative with
strong antiproliferative activity (IC … back the quest for new antibacterial agents to the forefront of …

Synthesis of Quinazolinone Based Spirocyclopropanes via [3 + 2] Cycloaddition Reaction: In Silico Anti-Tubercular Molecular Docking Studies and ADME …

BS Allaka, M Kanchrana, R Gamidi… - Polycyclic Aromatic …, 2023 - Taylor & Francis
… Citation 22 The natural alkaloid Phaitanthrin-A isolated from Phaius mishmensis, which
appears to be potent inhibitor of the life cycle of toxoplasma gondii with low host cell cytotoxicity ( …