Synthesis and antimicrobial activity of substituted indole hydrazides.
Journal name: World Journal of Pharmaceutical Research
Original article title: Synthesis, characterization and antimicrobial activity of some substituted 2-((1h-indol-4-yl)oxy)-n'- benzylideneacetohydrazide
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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Kumara Prasad S. A., Chethan S. H., Subrahmanyam E. V. S. and Shabaraya A. R.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synthesis, characterization and antimicrobial activity of some substituted 2-((1h-indol-4-yl)oxy)-n'- benzylideneacetohydrazide
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20178-9072
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Summary of article contents:
Introduction
The study reported by Kumara Prasad S. A. and colleagues focuses on the synthesis, characterization, and antimicrobial activity of substituted 2-((1H-indol-4-yl)oxy)-N'-benzylideneacetohydrazide derivatives. Schiff bases, which are significant due to their diverse biological activities, including antibacterial and antifungal properties, form the basis for this research. Given the prevalence of indole in pharmacologically relevant compounds, the authors aimed to develop new scaffolds combining indole and Schiff base systems to explore their potential as antimicrobial agents.
Synthesis and Characterization of Compounds
The synthesis process began with the reaction of 4-hydroxy indole with ethyl chloroacetate to produce ethyl 2-((1H-indol-4-yl)oxy)acetate, which subsequently reacted with hydrazine hydrate to yield 2-((1H-indol-4-yl)oxy)acetohydrazide. The condensation of this compound with various aldehydes resulted in the formation of substituted 2-((1H-indol-4-yl)oxy)-N'-benzylideneacetohydrazide derivatives (3a-j). The synthesized compounds were characterized through spectral data (IR and 1H NMR) to confirm their structures, with yields and melting points recorded for each derivative.
Antimicrobial Activity Evaluation
The antimicrobial potential of the synthesized compounds was assessed using in vitro methods. The broth microdilution method employed Mueller-Hinton agar to evaluate antibacterial activity against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Salmonella typhi and Escherichia coli) bacteria. The results indicated that several compounds exhibited significant antibacterial properties, with particular efficacy noted in those bearing chlorine, bromine, and nitro substituents. The antifungal activity of the compounds was also evaluated against Aspergillus niger and Candida albicans, demonstrating their potential as broad-spectrum antimicrobial agents.
Antibacterial and Antifungal Activity
Among the compounds synthesized, those with substitutions like p-chloro, p-nitro, p-dimethylamino, and p-methoxy showed the best antibacterial and antifungal activity. The synthesized compounds' effectiveness was compared to that of standard drugs, Ofloxacin for antibacterial activity and Fluconazole for antifungal activity. The resulting data illustrated the potency of the new derivatives at a concentration of 200 μg/ml, providing a basis for their potential use in pharmaceutical applications. The results confirmed that the incorporation of specific functional groups could enhance the biological activities of these derivatives.
Conclusion
The study concluded that the synthesized 2-((1H-indol-4-yl)oxy)-N'-benzylideneacetohydrazide derivatives exhibited promising antimicrobial activity against a range of bacteria and fungi. The results highlight the potential of these newly developed compounds as effective agents in combating microbial infections. Future research directions could explore the optimization of these compounds to enhance their potency and reduce side effects, ultimately contributing to the development of new therapeutic agents in pharmaceuticals. The authors acknowledge the support of the Srinivas College of Pharmacy and the Indian Institute of Sciences for assistance in spectral analysis.
FAQ section (important questions/answers):
What compounds were synthesized in this study?
The study synthesized substituted 2-((1H-indol-4-yl)oxy)-N'-benzylideneacetohydrazides (3a-j) from ethyl 2-((1H-indol-4-yl)oxy)acetate and various aldehydes.
What methods were used to characterize the synthesized compounds?
The synthesized compounds were characterized utilizing IR spectroscopy, 1H NMR spectroscopy, and thin-layer chromatography (TLC) to assess purity and structural integrity.
Which microbes were tested for antimicrobial activity?
The synthesized compounds were tested against Gram-positive bacteria (S. aureus, B. subtilis), Gram-negative bacteria (S. typhi, E. coli), and fungi (A. niger, C. albicans).
How was the antibacterial activity evaluated?
Antibacterial activity was evaluated using the broth microdilution method with Mueller-Hinton agar, measuring the zone of inhibition against various bacterial strains.
What were the findings regarding antimicrobial activity?
Many synthesized compounds exhibited good antimicrobial activity, especially those with chloro and nitro substitutions. Compound 3d showed particularly strong effects against tested microbes.
What acknowledgments were made in the study?
The authors thanked Management of Srinivas College of Pharmacy for support and Indian Institute of Sciences for conducting IR and NMR spectral analysis.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Synthesis and antimicrobial activity of substituted indole hydrazides.”. 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 effect exerted by compounds, particularly in terms of their capability to inhibit or kill microorganisms. In the context of pharmaceuticals and antimicrobial agents, understanding activity is crucial for assessing the effectiveness of synthesized compounds against pathogens, which informs drug development and therapeutic applications.
2) Antibiotic (Antibacterial):
Antibacterial pertains to substances that destroy or inhibit the growth of bacteria. Understanding antibacterial properties is essential in developing therapeutic agents that can combat bacterial infections. The study emphasizes the importance of discovering new antibacterial compounds to address rising antibiotic resistance issues in clinical settings and improve health outcomes.
3) Water:
Water acts as a universal solvent and plays a crucial role in biological systems, including chemical reactions involved in synthesis and purification processes. In the lab, it's used for dissolving substances, diluting compounds, and maintaining proper conditions for experiments. The quality and purity of water are vital for reproducible scientific results.
4) Table:
In scientific research, a table is used to systematically present data, such as results from experiments or studies. It helps in organizing complex information like antimicrobial activity data or physicochemical properties of synthesized compounds, making it easier for readers to understand results and comparisons among different substances.
5) Medium:
In microbiology, a medium refers to the nutrient solution that supports the growth of microorganisms. Different media are formulated based on the specific needs of bacteria or fungi being studied. The choice of medium influences the accuracy of the antimicrobial activity evaluation, making it essential for reliable experimental design.
6) Aureus:
Aureus, particularly referring to Staphylococcus aureus, is a significant pathogen responsible for various infections in humans. Its relevance in antimicrobial research stems from its widespread occurrence and the ability to develop resistance to antibiotics. Effective compounds against S. aureus are critical for treating infections and improving public health.
7) Drug:
A drug is any substance used to diagnose, cure, treat, or prevent disease. The development of new drugs, particularly antimicrobial agents, is vital for addressing health issues caused by bacterial and fungal infections. The synthesis and testing of novel compounds highlight the importance of drug discovery in pharmaceuticals.
8) Pharmacological:
Pharmacological relates to the study of drugs and their effects on biological systems. Understanding pharmacological properties is essential for assessing how new compounds interact with pathogens and the body. This knowledge underpins drug development processes and helps identify potential therapeutic uses of synthesized substances in clinical settings.
9) Karnataka:
Karnataka is a state in India known for its rich cultural heritage and educational institutions, including the Srinivas College of Pharmacy. The region contributes to pharmaceutical research and development, providing a fertile ground for innovation in drug synthesis and analysis, particularly in the context of antimicrobial agents.
10) Purity:
Purity indicates the absence of contaminants in a chemical substance and is crucial for confirming the identity and efficacy of synthesized compounds. High purity ensures that experimental results are reliable and reproducible, which is vital for assessing the biological activity of new drugs in research.
11) Kumara:
Kumara refers to one of the authors of the study, indicating the collaborative nature of scientific research. Researchers like Kumara contribute their expertise in drug synthesis and microbiological analysis, driving advancements in pharmaceutical sciences and the exploration of new antimicrobial agents in their respective fields.
12) India:
India is a country with a growing pharmaceutical industry and a strong emphasis on research and development. The country plays a significant role in global health initiatives, including the search for new antimicrobial compounds. The research conducted within its institutions contributes to advances in medical science and drug discovery.
13) Study (Studying):
A study refers to the systematic investigation of a specific subject or phenomenon, often involving experiments and data analysis. The study presented in the text emphasizes the synthesis and evaluation of new antimicrobial compounds, highlighting the importance of research in developing effective therapeutic agents for infectious diseases.
14) Discussion:
In the context of scientific research, discussion refers to the section where findings are analyzed and interpreted. This critical component allows researchers to contextualize results, draw conclusions, and suggest implications for future research and clinical applications, emphasizing the significance of the antimicrobial activities observed in the study.
15) Science (Scientific):
Science encompasses the systematic study of the structure and behavior of the physical and natural world through observation and experimentation. The research contributes to the body of scientific knowledge by exploring novel compounds for antimicrobial actions, highlighting the critical intersection of chemistry, biology, and pharmacology in drug development.
16) Nature:
Nature refers to the inherent qualities or characteristics of living organisms. In antimicrobial research, understanding the natural properties of compounds, including their interactions with pathogens, is essential for assessing their effectiveness as therapeutic agents. Nature's variability also drives the need for ongoing research in drug discovery.
17) Indian:
Indian in this context refers to the cultural and scientific contributions made by India in the field of pharmaceuticals and research. India is recognized for its significant role in drug development, where local researchers collaborate to address global health challenges through innovative solutions in antimicrobial therapy.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Synthesis and antimicrobial activity of substituted indole hydrazides.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Malaria, Antibacterial activity, Antimicrobial activity, Disc diffusion method, Zone of inhibition, Reference drug, Therapeutic areas, Mueller Hinton Agar, E. coli, TLC plate, DMSO, Chromatographic plate.