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. …
MDR-TB … with and without albumin, validating azaaurones as potent antimycobacterial agents. …
[HTML][HTML] Synthesis and anticancer cytotoxicity of azaaurones overcoming multidrug resistance
… 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,…
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 …
… 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 …
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 …
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…
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-…
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 …
… , 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…
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 …
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 ( …
appears to be potent inhibitor of the life cycle of toxoplasma gondii with low host cell cytotoxicity ( …