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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
Author(s) -
Rehman Tanzeel Ur.,
Riaz Sadaf,
Khan Islam Ullah,
Ashraf Muhammad,
Bajda Marek,
Gawalska Alicja,
Yar Muhammad
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700236
Subject(s) - acarbose , thiourea , ic50 , chemistry , enzyme , small molecule , stereochemistry , pyridine , type 2 diabetes mellitus , in vitro , biochemistry , diabetes mellitus , combinatorial chemistry , medicinal chemistry , organic chemistry , medicine , endocrinology
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 (IC 50 38.22 ± 0.12 μM), compounds 4i (IC 50 25.49 ± 0.67 μM), 4f (IC 50 28.91 ± 0.43 μM), 4h (IC 50 30.66 ± 0.52 μM), and 4e (IC 50 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.