Design, synthesis and biological evaluation of novel arylidine- malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B

Deora, Girdhar Singh, Karthikeyan, Chandrabose, Moorthy, N. S. Hari Narayana, Rathore, Vandana, Rawat, Arun K., Tamrakar, Akhilesh K., Srivastava, A. K. and Trivedi, Piyush (2013) Design, synthesis and biological evaluation of novel arylidine- malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B. Medicinal Chemistry Research, 22 11: 5344-5348. doi:10.1007/s00044-013-0528-1


Author Deora, Girdhar Singh
Karthikeyan, Chandrabose
Moorthy, N. S. Hari Narayana
Rathore, Vandana
Rawat, Arun K.
Tamrakar, Akhilesh K.
Srivastava, A. K.
Trivedi, Piyush
Title Design, synthesis and biological evaluation of novel arylidine- malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B
Journal name Medicinal Chemistry Research   Check publisher's open access policy
ISSN 1054-2523
1554-8120
Publication date 2013-11-01
Year available 2013
Sub-type Article (original research)
DOI 10.1007/s00044-013-0528-1
Open Access Status Not yet assessed
Volume 22
Issue 11
Start page 5344
End page 5348
Total pages 5
Place of publication Basel, Switzerland
Publisher Springer Basel AG
Language eng
Abstract In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake using L6 muscle cell lines and enzymatic assay against PTP1B. The biological activity results showed that the 2-methoxy substituted (14b) compound exhibited significant activity in both the assays. The unsubstituted compound (14a) also possessed comparable activity on glucose reuptake in L6 muscle cell lines and better inhibitory activity on PTP1B enzyme assays. Docking analysis was performed on the most potent compound of the series to understand the nature of interactions governing the binding of the designed molecule with the PTP1B enzyme.
Keyword Arylidine malononitrile
Diabetes
Docking study
Non-carboxylic acid inhibitors
Oxadiazole
PTP1B
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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