ArticleIranian journal of pharmaceutical research : IJPR2015
Design and Synthesis of New Benzimidazole and Pyrimidine Derivatives as α-glucosidase Inhibitor.
Article in Iranian journal of pharmaceutical research : IJPR, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed, 15 citations in OpenAlex.
- Targeted synthesis of a trimethoxyphenyltetrahydropyrimidine analogue designed as a DNA intercalator:RSC advances · 2025Article
- Unlocking the Pharmacological Potential of Benzimidazole Derivatives: A Pathway to Drug Development.Current topics in medicinal chemistry · 2024Review
- A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives.Frontiers in pharmacology · 2021Review
- Docking, Synthesis and Evaluation of the Antifungal Activity of Pyrimido [4,5-b]quinolins.Iranian journal of pharmaceutical research : IJPR · 2020Article
- Design and Synthesis of Some Novel Fluorobenzimidazoles Substituted with Structural Motifs Present in Physiologically Active Natural Products for Antitubercular Activity.Iranian journal of pharmaceutical research : IJPR · 2017Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In an endeavor to find a novel series of antihyperglycemic agents, new benzimidazole and pyrimidine derivatives were successfully synthesized efficiently in high yield with high purity, starting from amino acids in the presence of phosphorus oxychloride (POCl3). The synthesized compounds were identified by (1)H-NMR, (13)C-NMR, FT-IR spectroscopic techniques and elemental analysis. All products were assayed for their inhibitory effects on yeast and rat intestinal α-glucosidases. The results revealed that compounds with aromatic amino acids moiety showed significant inhibition activity on the tested enzymes. Among the benzimidazole derivatives 4c and 4d exhibited the best activity against both of the tested enzymes. Also, among the pyrimidine derivatives 5c and 5d possessed significant inhibition action on the enzymes. The IC50 values for the most potent benzimidazole yeast and intestinal α-glucosidases inhibitor (4d) were found to be 9.1 and 36.7 µM, respectively. The IC50 values for the inhibition of yeast and intestinal α-glucosidases by the most active pyrimidine compound (5d) were calculated to be 8.3 and 21.8 µM, respectively. Overall, this study proved that benzimidazole and pyrimidine derivatives with aromatic amino acids moieties can represent novel promising α-glucosidase inhibitors.
Indexed as
Identifiers
26330860PMC4518100W1926359026What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.