An efficient bio active synthesis of n-substituted acridine analogous

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: An efficient bio active synthesis of n-substituted acridine analogous
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:

Ch. Jyothi, B. Pryanka and N. Krishna Rao


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: An efficient bio active synthesis of n-substituted acridine analogous

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

Doi: 10.20959/wjpr20239-28357


Download the PDF file of the original publication


Summary of article contents:

1) Introduction

The synthesis of complex organic compounds plays a pivotal role in pharmaceutical development, particularly concerning the design of new bioactive molecules. In the article from the World Journal of Pharmaceutical Research, the authors, Ch. Jyothi, B. Pryanka, and N. Krishna Rao, delve into the efficient bioactive synthesis of N-substituted acridine analogues. This study highlights the significance of multicomponent reactions in achieving high atom economy while exploring the medicinal properties of acridine derivatives, which are noted for their antimalarial, antiviral, and anticancer activities. The research focuses on developing a novel method for synthesizing these compounds with exceptional yields, contributing to the field of medicinal chemistry.

2) Efficient Synthesis of Acridine Derivatives

The article demonstrates an advanced method for synthesizing N-alkyl acridine analogues through a three-component cyclocondensation reaction of 1,2-dicarbonyl compounds, like dimedone and chlorobenzaldehyde, in the presence of ammonium chloride and potassium periodate (KIO4). The researchers achieved this reaction without solvents, thus promoting an environmentally friendly approach to organic synthesis. By varying the benzyl bromides used alongside the acridine base, the study successfully produced a range of hybridized acridine derivatives, which were evaluated using various spectroscopic techniques. The methodology not only simplifies the synthesis process but also yields significant quantities of product in a shorter timeframe.

3) Antimicrobial Activity of Synthesized Compounds

The biological activity of the synthesized compounds was an integral part of this study, focusing on their antimicrobial properties. The study evaluated the in vitro antibacterial and antifungal activities of the novel acridine derivatives against several pathogenic strains, including Gram-positive and Gram-negative bacteria such as Staphylococcus aureus and Escherichia coli, as well as fungal strains like Aspergillus niger and Candida albicans. The results indicated that derivatives with electron-donating substituents generally exhibited better antimicrobial activity compared to those with electron-withdrawing groups, showcasing the influence of electronic effects on biological response.

4) Advantages of the Synthesis Method

A significant advantage of the presented synthesis method is its efficiency and cost-effectiveness, attributed largely to the use of KIO4 as a catalyst. This approach facilitates rapid reactions under mild conditions, yielding products in 85-92% efficiency. The study also emphasizes the ease of product isolation and purification through non-chromatographic methods. Thus, the procedure not only fulfills the needs of modern green chemistry by minimizing solvent use but also addresses the practical concerns of scalability and economic viability in the synthesis of complex organic molecules.

5) Conclusion

In conclusion, the research emphasizes the successful development of a streamlined and eco-friendly method for synthesizing N-substituted acridine derivatives while demonstrating their potential antimicrobial activities. The findings contribute valuable insights into the design of pharmacologically active compounds, reaffirming the advantages of utilizing multicomponent reactions in synthetic organic chemistry. By highlighting the relationship between substituent nature and antimicrobial efficacy, this work paves the way for future investigations into acridine derivatives, suggesting applications in drug development and therapeutic agents against resistant microbial strains. The authors express gratitude to their institution for support, underscoring the collaborative effort in advancing medicinal chemistry research.

FAQ section (important questions/answers):

What is the focus of the study presented in the article?

The study focuses on the efficient synthesis of N-substituted acridine analogs and evaluates their in vitro antimicrobial activity against various microbial strains.

What methods were used for the synthesis of acridine derivatives?

The acridine derivatives were synthesized using multicomponent reactions involving dimedone, chlorobenzaldehyde, and ammonium chloride under solvent-free conditions with KIO4 as a catalyst.

What significance do acridine derivatives have in medicinal chemistry?

Acridine derivatives possess numerous medicinal properties, including antimalarial, antiviral, antiallergic, and potent antitumor activities, making them valuable in drug development.

How were the synthesized compounds characterized in the study?

The compounds were characterized using advanced spectroscopic techniques, including 1H NMR, 13C NMR, IR spectroscopy, and LCMS, as well as elemental analysis.

What were the results of the antimicrobial activity evaluation?

The evaluation showed that compounds with electron-donating groups exhibited greater antimicrobial activity compared to those with electron-withdrawing groups against specified bacterial and fungal strains.

What conclusions were drawn from the synthesized acridine derivatives?

The study concluded that reaction conditions significantly influence yields, with electron-donating groups yielding better products and possessing higher antimicrobial activity.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “An efficient bio active synthesis of n-substituted acridine analogous”. 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:
In the context of this research, 'activity' pertains to the biological efficacy of the synthesized acridine derivatives. This includes assessing their potential antimicrobial effects against specific bacteria and fungi. The term underscores the primary aim of the study, which is to evaluate how well these compounds can perform against pathogens.

2) Antibiotic (Antibacterial):
'Anti-bacterial' refers to the ability of a substance to inhibit bacterial growth or kill bacteria. In this study, the efficacy of newly synthesized acridine derivatives was tested against various bacterial strains. This is crucial for identifying potential therapeutic agents that can combat bacterial infections effectively.

3) Water:
Water is a common solvent and is often used in chemical reactions and extractions. In this synthesis process, it assists in the neutralization and purification stages. Its role highlights the importance of solvent selection in chemical synthesis and reaction management, showcasing an environmentally-friendly approach.

4) Purification:
'Purification' is the process of isolating a desired product from a mixture of substances, which is critical in chemical synthesis. The study discusses the extraction and purification steps taken to isolate the synthesized acridine derivatives, ensuring that the final compounds are pure enough for biological testing and characterization.

5) Krishna (Krsna):
'Krishna' refers to one of the authors, N. Krishna Rao, who contributed to this research. This name connects the study to its authors and researchers, establishing credibility and allowing readers to find additional information on their background, expertise, and contributions to pharmaceutical research.

6) Andhra (Amdhra):
'Andhra' denotes the state of Andhra Pradesh in India, where the research was conducted, specifically at PRISM PG & DG College. The geographical context is significant as it emphasizes local research initiatives and educational institutions' role in advancing pharmaceutical chemistry and supporting scientific inquiry.

7) India:
'India' is the country where this research took place. Recognizing the country adds to the cultural and academic context of the study, suggesting that local resources and academic collaboration within India may influence the research direction and availability of certain compounds and materials for pharmaceutical studies.

8) Table:
The term 'table' refers to a presentation format used to summarize data, such as the antimicrobial activity of different compounds tested against various bacterial and fungal strains. Tables provide clear, organized information that enables researchers to compare results effectively and derive meaningful conclusions from the data.

9) Drug:
The term 'drugs' encompasses a broader range of chemical substances used to prevent, diagnose, or treat diseases than just 'drug.' In this research, it connects the synthesized acridine derivatives to their potential roles in medicine, underscoring the goal of developing effective therapeutic agents through chemical synthesis.

10) Discussion:
'Discussion' represents a section in academic papers where results are interpreted and implications are explored. In this study, it contains an analysis of the antimicrobial activities of synthesized compounds, highlighting their significance and potential applications in drug development, influencing future research directions based on these findings.

11) Heating:
'Heating' in this context refers to a method used to facilitate chemical reactions. It is an essential process in organic synthesis, including the preparation of acridine derivatives. Proper control of temperature during reactions can influence yields and reaction times, thus impacting overall synthetic efficiency.

12) Aureus:
'Aureus' refers to 'Staphylococcus aureus,' a common strain of bacteria against which the synthesized compounds were tested for antimicrobial activity. The relevance lies in its medical importance, as resistance to treatments involving this bacterium is a growing concern, emphasizing the need for novel antimicrobial agents from this study.

13) Study (Studying):
'Study' highlights the structured investigation conducted by the researchers focusing on the synthesis and evaluation of acridine derivatives. It frames the entire piece of research, encapsulating objectives, methods, and findings, thereby establishing the basis for understanding how these compounds can serve in pharmaceuticals.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘An efficient bio active synthesis of n-substituted acridine analogous’. Further sources in the context of Science might help you critically compare this page with similair documents:

Antimicrobial activities, Antimicrobial activity, In vitro, Biological Activity, Antifungal activity, TLC, Gram positive bacteria, Gram negative bacteria, Gram-positive and Gram-negative bacteria, Elemental analysis, In Vitro Antimicrobial Activity, Fungal activity.

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