Design and characterization of isoxazole-quinazolinone analogues.

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Design, synthesis and characterization of novel isoxazole-quinazolinone linked analogues as an antimicrobial agent
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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Original source:

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Author:

Dr. Komal R. Savaliya


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Design, synthesis and characterization of novel isoxazole-quinazolinone linked analogues as an antimicrobial agent

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr20233-27153


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Summary of article contents:

Introduction

The presented work details the design, synthesis, and characterization of novel isoxazole-quinazolinone linked analogues aimed at developing effective antimicrobial agents. Conducted by Dr. Komal R. Savaliya at the Indian Institute of Teacher Education, the study highlights a series of isoxazole derivatives synthesized from 6,8-dibromo-2-phenylquinazolin-4-one and hydroxylamine hydrochloride. The synthesized compounds were characterized using IR and NMR spectroscopy, and their antimicrobial properties were assessed against specific bacterial and fungal strains, revealing encouraging results relative to standard drugs.

Synthesis of Isoxazole Derivatives

The synthesis involved creating derivatives such as 6,8-dibromo-3-[4-(5-substitutedphenyl-1,2-oxazol-3-yl)phenyl]-2-phenylquinazolin-4-one, with the reaction carried out in dioxane using potassium hydroxide as a base. The procedures emphasized meticulous conditions, including refluxing, for up to 10 hours. Spectroscopic analysis provided confirmation of the chemical structures, demonstrating that most derivatives were synthesized with moderate to excellent yields. This synthetic route and characterization are crucial in establishing a foundation for further evaluating their pharmacological potential.

Antimicrobial Activity Evaluation

The antimicrobial activities of the synthesized compounds were rigorously analyzed. Compounds were screened for their ability to inhibit the growth of two bacteria: Staphylococcus aureus and Escherichia coli, and two fungal strains: Aspergillus niger and Saccharomyces. The results indicated that several derivatives displayed moderate to excellent activity compared to standard antibiotics like Streptomycin and antifungals like Fluconazole. Notably, compounds KS-2c and KS-2i exhibited the highest antibacterial efficacy against S. aureus and E. coli, respectively, suggesting their potential as viable alternatives in antimicrobial therapies.

Characterization Techniques

Characterization of the synthesized derivatives primarily involved infrared (IR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The IR spectroscopy data revealed important functional groups and structural characteristics of the compounds, while NMR provided insights into the molecular environments of hydrogen atoms within the structures. This analytical data supports the validity of the synthesized compounds' proposed molecular structures, reinforcing the reliability of the methodologies employed throughout the research.

Conclusion

In conclusion, the study successfully synthesized and characterized novel isoxazole-quinazolinone derivatives, which demonstrated promising antimicrobial activity against defined bacterial and fungal strains. The findings suggest that these compounds may serve as a foundation for further pharmacological research and development. The potential applications of isoxazole derivatives in antimicrobial therapies highlight the significance of ongoing research in heterocyclic chemistry and its implications in pharmaceutical innovation. The positive outcomes pave the way for further exploration and optimization of these compounds to enhance their therapeutic efficacy.

FAQ section (important questions/answers):

What is the main focus of Dr. Savaliya's research?

Dr. Savaliya's research focuses on designing, synthesizing, and characterizing novel isoxazole-quinozaline derivatives for potential antibacterial and antifungal applications.

What methods were used to evaluate the synthesized compounds?

The synthesized compounds were evaluated for antibacterial and antifungal activity using the Agar Cup method, comparing their effectiveness to standard drugs like Streptomycin and Fluconazole.

What solvents and reagents were used in this research?

Dioxane served as the solvent, and potassium hydroxide and hydroxylamine hydrochloride were used as reagents in the synthesis of the isoxazole derivatives.

How were the chemical structures of the compounds confirmed?

The chemical structures of the synthesized compounds were confirmed through infrared spectroscopy (IR) and proton nuclear magnetic resonance spectroscopy (1H-NMR) analyses.

Which compounds exhibited the highest antimicrobial activity?

Compounds KS-2c and KS-2b exhibited the highest antibacterial and antifungal activity, respectively, outperforming the standard drugs used for comparison in the study.

What potential applications do isoxazole derivatives have?

Isoxazole derivatives are promising due to their broad spectrum of biological activities, including antibacterial, antifungal, antiviral, and anticancer properties, making them useful in pharmaceuticals.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Design and characterization of isoxazole-quinazolinone analogues.”. 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:
The term 'Activity' refers to the effectiveness or biological response exhibited by synthesized compounds in pharmacological testing. In this context, antimicrobial activity represents how well the compounds can inhibit the growth of bacteria and fungi, which is critical for assessing potential therapeutic agents against infections.

2) Antibiotic (Antibacterial):
'Anti-bacterial', similar to antibacterial, emphasizes the action against bacteria. It reiterates the importance of compounds evaluated for their potential to combat bacterial infections, reinforcing the relevance of the synthesized analogues in offering alternative treatment options in the face of increasing antibiotic resistance globally.

3) Education:
In the context of this research, 'Education' reflects the academic environment where the study was conducted. The Centre of Education at the Indian Institute of Teacher Education indicates a strong foundation in scientific training, emphasizing the importance of scientific education in conducting impactful research in the pharmaceutical realm.

4) Aureus:
'Aureus' refers specifically to 'Staphylococcus aureus,' a significant bacterial pathogen analyzed for sensitivity to the synthesized compounds. Its inclusion in the study highlights the clinical relevance of targeting this resistant bacterium, which is known for causing various infections, thus underlining the importance of developing effective antibacterial agents.

5) Drug:
The plural term 'Drugs' indicates a broader collection of therapeutic agents, which may include the synthesized compounds and other established medications. This highlights the continuous effort in drug discovery to find new compounds, assessing their effectiveness compared to standard treatment options like Streptomycin and Fluconazole.

6) Indian:
'Indian' denotes the geographical and cultural origin of the research, indicating that the study is conducted within India. This aspect is significant as it may contribute to understanding local health issues and the necessity for novel pharmaceuticals that specifically address health concerns prevalent in the Indian population.

7) Table:
'Table' refers to the structured format utilized in scientific reporting to present data clearly. In this manuscript, tables summarize physical constants and antimicrobial activity results, facilitating easier comparison of compound performance, contributing to the transparency and reproducibility of research findings in medicinal chemistry.

8) India:
'India' is significant as it contextualizes the research setting, indicating that the scientific investigation and synthesis of new pharmaceutical compounds occur within Indian institutions. This can be pivotal for addressing specific health challenges faced by the country and fostering local advancements in drug development.

9) Field:
The term 'Field' reiterates the specific area of scientific inquiry, particularly emphasizing fields like medicinal or pharmaceutical chemistry. It underscores the interdisciplinary nature of research, integrating multiple aspects of science to innovate and improve therapeutic strategies and compounds to combat infectious diseases.

10) Purification:
'Purification' highlights the processes involved in isolating the synthesized compounds to ensure their suitability for biological testing. It is crucial in organic synthesis to achieve high-quality compounds, as impurities may affect pharmacological activity, thus impacting the reliability of tests conducted to evaluate their antimicrobial properties.

11) Discussion:
'Discussion' refers to the section in the research reporting that interprets the experimental results. This part provides insights into the significance of findings, correlates them with existing literature, and outlines the implications, limitations, and future directions of the study, framing it within the broader context of scientific inquiry.

12) Developing:
'Developing' signifies the active process of creating and synthesizing new compounds. In the research context, it emphasizes the importance of innovation and the continuous search for novel drugs that can effectively combat infections, addressing a critical need in the pharmaceutical industry and public health efforts.

13) Cancer:
'Cancer' may not be directly discussed in the present context but implies the broader spectrum of diseases that some synthesized compounds could potentially target. Understanding various disease mechanisms is essential for drug development, making it an important consideration in the design of new therapeutic agents.

14) Purity:
'Purity' refers to the quality of being free from contaminants or mixtures. It is vital in pharmaceutical research to ensure that synthesized compounds are pure as impurities can affect efficacy and safety, influencing the outcomes of the antimicrobial tests performed in the study.

15) Water:
'Water' is implicitly mentioned in the context of washing and recrystallization processes during the purification of compounds. It highlights the importance of solvents in the synthesis and crystallization steps, emphasizing the necessity of proper laboratory techniques in achieving suitable compounds for further testing.

16) Study (Studying):
'Study' indicates the methodical investigation performed to explore the synthesis and evaluation of new compounds. It stresses the research's scientific rigor, contributing to a deeper understanding of new derivatives’ antimicrobial properties and their potential applications in treating infections effectively.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Design and characterization of isoxazole-quinazolinone analogues.’. Further sources in the context of Science might help you critically compare this page with similair documents:

Antibacterial activity, Antioxidant activity, Thin Layer Chromatography, Antimicrobial activity, Anticancer activity, Zone of inhibition, Antimicrobial agent, Antifungal activity, Antiviral activity, Staphylococcus aureus, Escherichia coli, Yield percentage, Analytical data, Standard drug, Aspergillus niger, Chemical structure, Melting point, Infrared spectroscopy, Biological activities, Analytical reagent grade, Spectral analysis, Potassium hydroxide, Antiproliferative activity.

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