Article (Scientific journals)
New MraYAA Inhibitors with an Aminoribosyl Uridine Structure and an Oxadiazole
Wan, Hongwei; Ben Othman, Raja; Le Corre, Laurent et al.
2022In Antibiotics, 11 (9), p. 1189
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Keywords :
Pharmacology (medical); Infectious Diseases; Microbiology (medical); General Pharmacology, Toxicology and Pharmaceutics; Biochemistry; Microbiology
Abstract :
[en] New inhibitors of the bacterial transferase MraY from Aquifex aeolicus (MraYAA), based on the aminoribosyl uridine central core of known natural MraY inhibitors, have been designed to generate interaction of their oxadiazole linker with the key amino acids (H324 or H325) of the enzyme active site, as observed for the highly potent inhibitors carbacaprazamycin, muraymycin D2 and tunicamycin. A panel of ten compounds was synthetized notably thanks to a robust microwave-activated one-step sequence for the synthesis of the oxadiazole ring that involved the O-acylation of an amidoxime and subsequent cyclization. The synthetized compounds, with various hydrophobic substituents on the oxadiazole ring, were tested against the MraYAA transferase activity. Although with poor antibacterial activity, nine out of the ten compounds revealed the inhibition of the MraYAA activity in the range of 0.8 µM to 27.5 µM.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Wan, Hongwei
Ben Othman, Raja
Le Corre, Laurent 
Poinsot, Mélanie
Oliver, Martin 
Amoroso, Ana Maria  ;  Université de Liège - ULiège > Département des sciences de la vie > Centre d'Ingénierie des Protéines (CIP)
Joris, Bernard ;  Université de Liège - ULiège > Département des sciences de la vie
Touzé, Thierry
Auger, Rodolphe
Calvet-Vitale, Sandrine 
Bosco, Michaël 
Gravier-Pelletier, Christine 
Language :
English
Title :
New MraYAA Inhibitors with an Aminoribosyl Uridine Structure and an Oxadiazole
Publication date :
02 September 2022
Journal title :
Antibiotics
eISSN :
2079-6382
Publisher :
MDPI AG
Volume :
11
Issue :
9
Pages :
1189
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
MESR - France. Ministère de l'Enseignement supérieur et de la Recherche [FR]
CNRS - Centre National de la Recherche Scientifique [FR]
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since 21 September 2022

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