Synthesis and characterization of chalcones and dihydropyrimidinones
Journal name: World Journal of Pharmaceutical Research
Original article title: Synthesis, characterization and anti oxidant activity of novel chalcones and di hydro pyrimidinenones derivatives
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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P. S. Raghu
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synthesis, characterization and anti oxidant activity of novel chalcones and di hydro pyrimidinenones derivatives
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201714-10680
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Summary of article contents:
Introduction
The research paper discusses the synthesis, characterization, and antioxidant activity of novel chalcones and dihydropyrimidinone derivatives conducted by P.S. Raghu at the University College of Pharmaceutical Sciences, Sri Krishnadevaraya University. Chalcones have garnered attention in the scientific community due to their broad spectrum of biological activities, including antioxidant, antiulcer, antimalarial, and antimicrobial properties. This study aims to evaluate newly synthesized chalcones and their transition into pyrimidinone derivatives while assessing their potential antioxidant activity using DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assays.
Synthesis of Chalcones and Pyrimidinones
The initial step in the research involved synthesizing novel chalcones by condensing 1-(2-chlorophenyl) ethanone with various aromatic aldehyde derivatives using dilute ethanolic sodium hydroxide at room temperature. This follows the Clasein-Schmidt condensation reaction protocol. The synthesized chalcones were then reacted with urea and ethanol, which resulted in the formation of the corresponding pyrimidinone derivatives. Characterization of these compounds was performed using IR and ^1H NMR spectroscopy, confirming the structures based on their spectral data.
Antioxidant Activity Evaluation
The antioxidant capacity of both chalcone and pyrimidinone derivatives was assessed using the DPPH method. In this evaluation, different concentrations of the synthesized compounds were tested against a DPPH solution to determine their ability to scavenge free radicals. The percentage of inhibition was calculated, revealing the efficiency of these compounds compared to the standard ascorbic acid. The study indicated that certain derivatives showed promising antioxidant activity, highlighting the potential therapeutic benefits of these novel compounds.
Results and Comparative Analysis
The results indicated varying levels of antioxidant activity among the synthesized compounds. For instance, certain chalcones and pyrimidinones demonstrated inhibition percentages ranging from 51% to 88%. Notably, compound CP02 exhibited the highest antioxidant activity at 88%, while ascorbic acid showed a 48% inhibition rate. The compounds containing electron-donating groups (like OCH₃ and OH) were associated with enhanced antioxidant activity, suggesting that substituent effects play a significant role in the biological efficacy of these derivatives.
Conclusion
The findings indicate that both the chalcone and dihydropyrimidinone derivatives synthesized possess significant in vitro antioxidant activities, particularly those with electron-releasing substituents. This research underscores the potential of these compounds in the development of antioxidant agents for therapeutic interventions. The study not only contributes to the field of medicinal chemistry but also paves the way for future research aiming at synthesizing and testing similar novel compounds for various biological activities. Gratitude is expressed towards the university authorities for their support throughout the research process.
FAQ section (important questions/answers):
What are chalcones and why are they significant in research?
Chalcones are synthetic compounds known for various biological activities, including antioxidant, anti-inflammatory, and antimicrobial properties, making them significant for disease treatment and medicinal chemistry.
How were the novel chalcones synthesized in this study?
The novel chalcones were synthesized by condensing 1-(2-chlorophenyl)ethanone with aromatic aldehydes in a dilute ethanolic sodium hydroxide solution following the Clasein-Schmidt condensation reaction at room temperature.
What method was used to test antioxidant activity?
The antioxidant activity was assessed using the DPPH method, involving measuring the inhibition of DPPH free radicals. Results were compared with standard ascorbic acid.
What were the main findings regarding antioxidant activity?
The synthesized chalcone and pyrimidinone derivatives showed significant antioxidant activity, with some compounds exhibiting better activity than the standard ascorbic acid.
What is the role of the electron groups in antioxidant activity?
Compounds with electron-releasing groups, like OCH3 and OH, demonstrated maximal antioxidant activity, suggesting that the electronic properties of substituents influence their antioxidant potential.
Who is the corresponding author of the study?
The corresponding author is Dr. P. S. Raghu from the University College of Pharmaceutical Sciences, Sri Krishnadevaraya University.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Synthesis and characterization of chalcones and dihydropyrimidinones”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Activity:
Activity refers to the biological efficacy of the synthesized compounds, specifically their antioxidant and antimicrobial properties. In the context of the research, antioxidant activity is measured using the DPPH method, highlighting how well these compounds can inhibit free radicals, akin to how ascorbic acid is utilized as a standard.
2) Raghu:
Raghu refers to Dr. P. S. Raghu, the primary author of the research, who conducted the study at the University College of Pharmaceutical Sciences, Sri Krishnadevaraya University. His work focuses on the synthesis of novel chalcones and pyrimidinones and their biological evaluations, contributing to advancements in pharmaceutical research.
3) Krishnadevaraya:
Krishnadevaraya is part of the full name of Sri Krishnadevaraya University, located in Andhra Pradesh, India. This institution is notable for its contributions to higher education in the fields of science and technology. Dr. Raghu's research is conducted under its auspices, highlighting the university's role in supporting pharmaceutical studies.
4) Science (Scientific):
Science encompasses the systematic study of nature and its phenomena, including the synthesis and characterization of new chemical compounds. In this research, scientific methods are applied to understand the biological activity of novel chalcones and pyrimidinones, bridging theoretical knowledge with practical applications in drug development.
5) Water:
Water is a solvent used in various chemical reactions, including the synthesis processes described in the study. It plays a crucial role in facilitating reactions, purifying compounds, and conducting experiments. Its properties as a solvent enhance the efficacy and outcomes of the chemical methodologies employed in the research.
6) Antibiotic (Antibacterial):
Antibacterial refers to the properties of certain compounds to inhibit the growth of bacteria, which is integral to the study's focus on biological activities of synthesized chalcones and pyrimidinones. These compounds may exhibit significant antibacterial effects, contributing to their potential therapeutic capabilities against various bacterial infections.
7) Performance:
Performance relates to the efficacy of the synthesized compounds in exhibiting antioxidant and antibacterial activities. The research evaluates the performance of these compounds against established standards like ascorbic acid, showcasing their potential effectiveness in therapeutic applications and highlighting the importance of performance metrics in drug development.
8) Discussion:
Discussion refers to the section of the research where the results are analyzed and interpreted in the context of existing literature. It elucidates the implications of the findings on antioxidant activity, highlights comparisons with standard compounds, and provides insights into the structure-activity relationship of the synthesized derivatives.
9) Disease:
Disease represents the health conditions that the synthesized compounds aim to address, including conditions requiring antioxidant and antimicrobial treatment. The research is motivated by the need for novel therapeutic agents to combat various diseases, emphasizing the role of pharmaceutical research in the discovery of effective treatments.
10) Nature:
Nature, in the context of this research, refers to the intrinsic qualities and behaviors of the chemical compounds synthesized in the study. It encompasses their biological activities and interactions with the environment, specifically how these novel compounds behave concerning their antioxidant and antimicrobial properties.
11) Table:
Table refers to the organized presentation of results, specifically the quantitative data depicting the antioxidant activity of various synthesized compounds. Tables facilitate comparisons and provide clear insights into the research findings, enabling readers to quickly grasp the results of the experimental evaluations conducted.
12) Babu:
Babu is a reference to Prof. Sudhakar Babu, who is acknowledged in the research as part of the support system at Sri Krishnadevaraya University. His contributions to the institution and facilitation of research endeavors illustrate the collaborative environment that fosters scientific inquiry and innovation.