Synthesis and evaluation of the antimicrobial activity of novel quinazolinones.
A simple and efficient microwave-assisted methodology for regioselective alkylation of exocyclic nitrogen of cyclic amidines was developed and novel N-alkylated 3,4-dihydropyrazino [2,1-b] quinazolin-6-ones were prepared. Although none of the molecules tested have any specific anti-quorum sensing (-QS) activity, our result validates the growth tests devised to control the bias of the anti-QS tests. Among the molecules studied, compound 2b exhibits interesting activity against the Gram-negative bacteria Escherichia coli and Shigella sonnei.
Laboratoire de Biotechnologies et Chimie Bio-organique, FRE CNRS 2766, UFR Sciences Fondamentales et Sciences pour l'Ingénieur, Bâtiment Marie Curie, Université de la Rochelle, F-1 7042 La Rochelle cedex 1, France.
Maria De Fatima
Mde F
Pereira
Romain
R
Chevrot
Eric
E
Rosenfeld
Valerie
V
Thiery
Thierry
T
Besson
D000478:Alkylation; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D008872:Microwaves; D015394:Molecular Structure; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D053038:Quorum Sensing / Q000187:drug effects; D012764:Shigella sonnei / Q000187:drug effects*
D000890:Anti-Infective Agents; D052999:Quinazolinones