Polyheterocyclic peptidomimetics: Parallel solid phase synthesis of oligo cyclic guanidines and their inhibition activity against Mycobacterium tuberculosis DNA gyrase.
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 09 2023
01 09 2023
Historique:
received:
11
07
2023
revised:
01
08
2023
accepted:
06
08
2023
medline:
21
8
2023
pubmed:
10
8
2023
entrez:
9
8
2023
Statut:
ppublish
Résumé
Polyheterocycles are one of the most desired synthetic targets due to their numerous and valuable applications in various fields. We report the design and the parallel synthesis of novel linear oligocyclic guanidine peptidomimetics from predesigned reduced polyamides. A screening of these compounds identified active Mycobacterium tuberculosis DNA gyrase inhibitors which do not inhibit human DNA topoisomerase IIα and topoisomerase I.
Identifiants
pubmed: 37557925
pii: S0960-894X(23)00317-7
doi: 10.1016/j.bmcl.2023.129439
pii:
doi:
Substances chimiques
DNA Gyrase
EC 5.99.1.3
Peptidomimetics
0
Guanidines
0
Topoisomerase II Inhibitors
0
Guanidine
JU58VJ6Y3B
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
129439Subventions
Organisme : NIAID NIH HHS
ID : R21 AI137721
Pays : United States
Organisme : NIAID NIH HHS
ID : R21 AI178134
Pays : United States
Informations de copyright
Copyright © 2023 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.