Amidinoquinoxaline N-oxides: synthesis and activity against anaerobic bacteria.

ABSTRACT: We present herein an in-depth study on the activity of amidinoquinoxaline N-oxides 1 against Gram-positive and Gram-negative anaerobic bacteria. Based on 5-phenyl-2,3-dihydropyrimidoquinoxaline N-oxide 1a, the selected structural variations included in our study comprise the substituents α- to the N-oxide function, the benzofused ring, substitution and quaternization of the amidine moiety, and the amidine ring size. Compounds 1 showed good to excellent antianaerobic activity, evaluated as the corresponding CIM₅₀ and CIM₉₀ values, and an antimicrobial spectrum similar to metronidazole. Six out of 13 compounds 1 had CIM₉₀ values significantly lower than the reference drug. Among them, imidazoline derivatives 1i-l were the most acti

SUBMITTER: Gruber N 

PROVIDER: S-EPMC10498151 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature