Synthesis, In-vitro evaluation and molecular docking studies of oxoindolin phenylhydrazine carboxamides as potent and selective inhibitors of ectonucleoside triphosphate diphosphohydrolase (NTPDase).
Carboxamide
Isatin
Molecular docking
Nucleoside triphosphate diphosphohydrolase inhibitors
Oxoindolin
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
07 2021
07 2021
Historique:
received:
23
02
2021
revised:
13
04
2021
accepted:
28
04
2021
pubmed:
22
5
2021
medline:
25
2
2023
entrez:
21
5
2021
Statut:
ppublish
Résumé
Members of the ectonucleoside triphosphate diphosphohydrolases (NTPDases) constitute the major family of enzymes responsible for the maintenance of extracellular levels of nucleotides and nucleosides by catalyzing the hydrolysis of nucleoside triphosphate (NTP) and nucleoside diphosphates (NDP) to nucleoside monophosphate (NMP). Although, NTPDase inhibitors can act as potential drug candidates for the treatment of various diseases, there is lack of potent as well as selective inhibitors of NTPDases. The current study describes the synthesis of a number of carboxamide derivatives that were tested on recombinant human (h) NTPDases. The most promising inhibitors were 2h (h-NTPDase1, IC
Identifiants
pubmed: 34020240
pii: S0045-2068(21)00334-5
doi: 10.1016/j.bioorg.2021.104957
pii:
doi:
Substances chimiques
Enzyme Inhibitors
0
Indoles
0
Phenylhydrazines
0
Adenosine Triphosphatases
EC 3.6.1.-
ectoATPase
EC 3.6.1.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104957Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.