Novel substituted 3-phenyl 1-(4-(5-bromopyridin-3-yl)-6-phenylpyrimidin-2-yl)-thiourea compounds as key small organic molecules for the potential treatment of type II diabetes mellitus: in vitro studies against yeast α-glucosidase

In this paper, we report a series of eighteen novel pyrimidine-based thiourea compounds with good to excellent yields (61–88%). The chemical structures of these heterocycles consist of a central pyrimidine ring with phenyl-substituted thiourea motifs. The enzyme inhibitory potential of these compoun...

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Bibliographic Details
Published in:Medicinal chemistry research 2017-06, Vol.26 (6), p.1098-1106
Main Authors: Ur Rehman, Tanzeel, Ullah Khan, Islam, Riaz, Sadaf
Format: Article
Language:English
Subjects:
Acarbose
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Diabetes mellitus
Organic chemistry
Original Research
Pharmacology/Toxicology
Therapeutic applications
Thiourea
α-Glucosidase
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Summary:In this paper, we report a series of eighteen novel pyrimidine-based thiourea compounds with good to excellent yields (61–88%). The chemical structures of these heterocycles consist of a central pyrimidine ring with phenyl-substituted thiourea motifs. The enzyme inhibitory potential of these compounds was investigated against α-glucosidase as this enzyme plays a crucial role in treating type II diabetes mellitus. Compounds 4i (IC 50  = 22.46 ± 0.65 µM), 4f (IC 50  = 25.88 ± 0.40 µM), 4h (IC 50  = 27.63 ± 0.49 µM ) , 4c (IC 50  = 29.47 ± 0.42 µM), and 4e (IC 50  = 32.01 ± 0.42 µM) delivered better inhibition than the reference compound acarbose (IC 50 38.22 ± 0.12 µM). The quantitative structure–activity relationship of the synthesized compounds was also studied.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-017-1803-3