Novel pyridine‐2, 4, 6‐tricarbohydrazide thiourea compounds as small key organic molecules for the potential treatment of type‐2 diabetes mellitus: In vitro studies against yeast α‐ and β‐glucosidase and in silico molecular modeling. Issue 1 (1st December 2017)

• Record Type: Journal Article
• Authors: Rehman, Tanzeel Ur.; Riaz, Sadaf; Khan, Islam Ullah; Ashraf, Muhammad; Bajda, Marek; Gawalska, Alicja; Yar, Muhammad
• Is Part Of: Archiv der Pharmazie. Volume 351:Issue 1(2018)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2017-12-01
• Subjects: 2, 4, 6‐tricarbohydrazide -- α‐glucosidase -- acarbose -- diabetes mellitus type‐2 -- pyridine derivatives -- thiourea; Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201700236
• Languages: English
• ISSNs: 0365-6233

Abstract

Abstract: A range of novel pyridine‐2, 4, 6‐tricarbohydrazide thiourea compounds (4a–i ) were synthesized in good to excellent yields (63–92%). The enzyme inhibitory potentials of these compounds were investigated against α‐ and β‐glucosidases because these enzymes play a crucial role in treating type‐2 diabetes mellitus (T2DM). As compared to the reference compound acarbose (IC50 38.22 ± 0.12 μM), compounds4i (IC50 25.49 ± 0.67 μM), 4f (IC50 28.91 ± 0.43 μM), 4h (IC50 30.66 ± 0.52 μM), and4e (IC50 35.01 ± 0.45 μM) delivered better inhibition against α‐glucosidase and were quite inactive/completely inactive against β‐glucosidase. The structure–activity relationship of these compounds was developed and elaborated with the help of molecular docking studies. Abstract : Novel pyridine‐2, 4, 6‐tricarbohydrazide thiourea compounds (4a–i ) were synthesized and tested for their inhibitory activities against α‐ and β‐glucosidases. Compounds4e, 4f, 4h, and4i showed better inhibition against α‐glucosidase than the reference compound acarbose and were inactive against β‐glucosidase. Molecular docking studies revealed the structure–activity relationship of these compounds.