New barbiturates and thiobarbiturates as potential enzyme inhibitors

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Biochemistry

Background:

• Barbiturates and thiobarbiturates are classes of compounds with diverse biological activities.
• Developing novel synthetic routes for these compounds is crucial for drug discovery.
• Exploring new chemical entities for therapeutic applications remains an active research area.

Purpose of the Study:

• To synthesize a novel series of barbiturate and thiobarbiturate derivatives.
• To evaluate the in vitro biological activities of the synthesized compounds, including antioxidant, enzyme inhibition, and anti-urease properties.

Main Methods:

• Multi-component reaction for the synthesis of 27 new barbiturates and thiobarbiturates.
• Characterization using Nuclear Magnetic Resonance (1H, 13C NMR), Electron Ionization Mass Spectrometry (EIMS), and elemental analysis (C, H, N, S).
• In vitro screening assays for DPPH radical scavenging (antioxidant), lipoxygenase, chymotrypsin, α-glucosidase, and anti-urease activities.

Main Results:

• Successful synthesis of 27 new compounds in excellent yields (87-96%).
• Compounds were fully characterized by spectroscopic and analytical methods.
• Significant in vitro activities were observed: 23 compounds showed DPPH radical scavenging activity, 14 inhibited lipoxygenase, and 2 inhibited chymotrypsin.

Conclusions:

• The developed multi-component reaction provides an efficient route to novel barbiturate and thiobarbiturate analogs.
• Several synthesized compounds exhibit promising antioxidant and enzyme inhibitory profiles, warranting further investigation.
• This study expands the chemical space of barbiturates and thiobarbiturates with potential therapeutic applications.