Mutually Isomeric 2- and 4-(3-nitro-1,2,4-triazol-1-yl)pyrimidines Inspired by an Antimycobacterial Screening Hit: Synthesis and Biological Activity against the ESKAPE Panel of Pathogens.
3-nitro-1,2,4-triazole
ESKAPE pathogens
antimycobacterial activity
bioreducible prodrugs
cyclic voltammetry
nitroazoles
nucleophilic aromatic substitution
reversible single-electron reduction
Journal
Antibiotics (Basel, Switzerland)
ISSN: 2079-6382
Titre abrégé: Antibiotics (Basel)
Pays: Switzerland
ID NLM: 101637404
Informations de publication
Date de publication:
01 Oct 2020
01 Oct 2020
Historique:
received:
06
09
2020
revised:
24
09
2020
accepted:
30
09
2020
entrez:
6
10
2020
pubmed:
7
10
2020
medline:
7
10
2020
Statut:
epublish
Résumé
Starting from the structure of antimycobacterial screening hit OTB-021 which was devoid of activity against ESKAPE pathogens, we designed, synthesized and tested two mutually isomeric series of novel simplified analogs, 2- and 4-(3-nitro-1,2,4-triazol-1-yl)pyrimidines, bearing various amino side chains. These compounds demonstrated a reverse bioactivity profile being inactive against
Identifiants
pubmed: 33019787
pii: antibiotics9100666
doi: 10.3390/antibiotics9100666
pmc: PMC7601023
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Ministry of Science and Higher Education of the Russian Federation
ID : 14.W03.031.0025
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