Bisthioureas of pimelic acid and 4-methylsalicylic acid derivatives as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP): Synthesis and molecular docking studies.
Alkaline phosphatase inhibitors
Pimelic acid
Salicylic acid
Thiourea
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
18
04
2020
revised:
27
05
2020
accepted:
02
06
2020
pubmed:
22
6
2020
medline:
30
3
2021
entrez:
22
6
2020
Statut:
ppublish
Résumé
Alkaline phosphatases (ALPs) are membrane bound metalloenzymes, distributed all over the body. Recent studies have revealed that by targeting ALPs can lead towards the treatment of many deadliest diseases including cardiac, cancerous and brain diseases. Thioureas and their derivatives are of considerable significance and are privileged scaffolds in medicinal chemistry. They show a wide range of pharmacological activities such as antibacterial, antiparasitic, anti-inflammatory and antioxidants etc. On the other hand, salicylic acid and its derivatives are known for its broad spectrum of activities. The work presented comprises of synthesis of N-acyl-N'-aryl substituted bisthioureas of pimelic acid (1-7) and 3,5-dimethyl pyrazole (11), 1-aroyl-3-aryl thiourea (12) and 1,3,4-oxadiazole (13) derivatives of 4-methyl salicylic acid. Structures of all the synthesized compounds were characterized by FT-IR and
Identifiants
pubmed: 32563965
pii: S0045-2068(20)31293-1
doi: 10.1016/j.bioorg.2020.103996
pii:
doi:
Substances chimiques
Enzyme Inhibitors
0
Pimelic Acids
0
Salicylates
0
Alkaline Phosphatase
EC 3.1.3.1
Thiourea
GYV9AM2QAG
methyl salicylate
LAV5U5022Y
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103996Informations de copyright
Copyright © 2020. Published by Elsevier Inc.
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.