Dihydropyrimidinone scaffold and potential therapeutic targets

Kumar, Adarsh; Singh, Ankit Kumar; Vijayan, Veena; Singh, Harshwardhan; Verma, Amita; Kumar, Pradeep

doi:10.1016/b978-0-443-19094-0.00004-7

Dihydropyrimidinones as Potent Anticancer Agents 2023

DOI: 10.1016/b978-0-443-19094-0.00004-7

|View full text |Cite

Dihydropyrimidinone scaffold and potential therapeutic targets

Adarsh Kumar,

Ankit Kumar Singh,

Veena Vijayan

et al.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2024

Publication Types

Select...

Article2

Relationship

Self Cite0

Independent2

Authors

Journals

Cited by 2 publications

References 82 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Exploring dihydropyrimidone derivatives as modulators of carbohydrate catabolic enzyme to mitigate diabetes

Ali,

Mansoor,

Albaayit

et al. 2024

Sci Rep

View full text Add to dashboard Cite

Diabetes is a prevalent and serious metabolic disorder affecting millions globally, and it poses extensive health risks due to elevated blood glucose levels. One promising approach for managing diabetes is the inhibition of α-glucosidase, an enzyme that plays a crucial role in carbohydrate metabolism. Targeting α-glucosidase can help delay glucose absorption, thus controlling postprandial blood sugar spikes. Dihydropyrimidones, a core structural class present in various biologically active natural compounds, have been recognized for their diverse therapeutic potential, including anti-diabetic properties. In this study, we evaluated a library of previously synthesized 37 Dihydropyrimidone derivatives to assess their potential as α-glucosidase inhibitors. We identified 34 derivatives with significant inhibitory activity, exhibiting IC 50 values in the range of 5.30–56.72 µM. Among these, compounds 2 , 4 – 7 , 9 – 11 , 13 – 16 , 31 , 32 , and 33 demonstrated high potency, with IC 50 values below 20 µM; the most active compound, 5 , achieved an IC 50 of 5.30 µM. A detailed kinetic study on compound 5 revealed a competitive inhibition mode with a Ki value of 16.10 ± 0.0075 µM. Additionally, cytotoxicity assays confirmed that compound 5 is non-toxic to BJ cell lines, underscoring its safety for therapeutic use. The computational studies further supported the inhibitory potential by illustrating key interactions and binding affinities between the Dihydropyrimidone derivatives and the α-glucosidase, highlighting these compounds as promising candidates for diabetes management.

show abstract

Exploring dihydropyrimidone derivatives as modulators of carbohydrate catabolic enzyme to mitigate diabetes

Ali,

Mansoor,

Albaayit

et al. 2024

Sci Rep

View full text Add to dashboard Cite

show abstract

Green and sustainable synthesis of 3,4-Dihydropyrimidin-2(1H)-ones/thiones via the Biginelli reaction using L-arabinose as a renewable catalyst under solvent-free conditions

Saroj,

Ponugoti,

Sawant

et al. 2024

Synthetic Communications

View full text Add to dashboard Cite

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Dihydropyrimidinone scaffold and potential therapeutic targets

Cited by 2 publications

References 82 publications

Exploring dihydropyrimidone derivatives as modulators of carbohydrate catabolic enzyme to mitigate diabetes

Exploring dihydropyrimidone derivatives as modulators of carbohydrate catabolic enzyme to mitigate diabetes

Green and sustainable synthesis of 3,4-Dihydropyrimidin-2(1H)-ones/thiones via the Biginelli reaction using L-arabinose as a renewable catalyst under solvent-free conditions

Contact Info

Product

Resources

About