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.


Journal

Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703

Informations de publication

Date de publication:
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

103996

Informations 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.

Auteurs

Amara Mumtaz (A)

Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan. Electronic address: amaramumtaz@cuiatd.edu.pk.

Kiran Saeed (K)

Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan.

Abid Mahmood (A)

Center for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan.

Sumera Zaib (S)

Center for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan.

Aamer Saeed (A)

Department of Chemistry, Quaid-i-Azam University Islamabad, Pakistan.

Julie Pelletier (J)

Centre de Recherche du CHU de Québec - Université Laval, Québec, QC G1V 4G2, Canada.

Jean Sévigny (J)

Centre de Recherche du CHU de Québec - Université Laval, Québec, QC G1V 4G2, Canada; Département de Microbiologie-infectiologie et d'immunologie, Faculté de Médecine, Université Laval, Québec, QC G1V 0A6, Canada.

Jamshed Iqbal (J)

Center for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 22060, Pakistan. Electronic address: drjamshed@cuiatd.edu.pk.

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Classifications MeSH