HIV and fungal priority pathogens

Sati, Hatim; Alastruey-Izquierdo, Ana; Perfect, John; Govender, Nelesh P; Harrison, Tom S; Chiller, Tom; Sorrell, Tania C; Bongomin, Felix; Oladele, Rita; Chakrabarti, Arunaloke; Wahyuningsih, Retno; Colombo, Arnaldo Lopes; Rodriguez-Tudela, Juan Luis; Beyrer, Chris; Ford, Nathan

doi:10.1016/s2352-3018(23)00174-1

Cited by 7 publications

(1 citation statement)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…One of the major concerns is about methicillin resistant Staphylococcus aureus (MRSA), but also other Gram-positive and Gram-negative species such as Acinetobacter baumannii, Pseudomonas aeruginosa or Klebsiella pneumoniae [2]. In addition to bacteria, fungi (filamentous fungi such as Aspergillus fumigatus, as well as yeasts such as Candida species and Cryptococcus neoformans) are also responsible for deadly infections, particularly in HIV-infected patients, but also in immunocompetent ones, affecting billions of patients and causing more than 1.5 million deaths per year [3][4][5][6]. Some natural plant molecules and/or their derivatives, including flavonoids, have been reported to possess strong antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%

Design and Synthesis of Novel Amino and Acetamidoaurones with Antimicrobial Activities

Di Maio,

Olleik,

Courvoisier-Dezord

et al. 2024

Antibiotics

View full text Add to dashboard Cite

The development of new and effective antimicrobial compounds is urgent due to the emergence of resistant bacteria. Natural plant flavonoids are known to be effective molecules, but their activity and selectivity have to be increased. Based on previous aurone potency, we designed new aurone derivatives bearing acetamido and amino groups at the position 5 of the A ring and managing various monosubstitutions at the B ring. A series of 31 new aurone derivatives were first evaluated for their antimicrobial activity with five derivatives being the most active (compounds 10, 12, 15, 16, and 20). The evaluation of their cytotoxicity on human cells and of their therapeutic index (TI) showed that compounds 10 and 20 had the highest TI. Finally, screening against a large panel of pathogens confirmed that compounds 10 and 20 possess large spectrum antimicrobial activity, including on bioweapon BSL3 strains, with MIC values as low as 0.78 µM. These results demonstrate that 5-acetamidoaurones are far more active and safer compared with 5-aminoaurones, and that benzyloxy and isopropyl substitutions at the B ring are the most promising strategy in the exploration of new antimicrobial aurones.

show abstract

Section: Introductionmentioning

confidence: 99%