Characterization and antimicrobial activity of new benzimidazoles.
Journal name: World Journal of Pharmaceutical Research
Original article title: Characterization and antimicrobial activity of newly synthesized benzimidazolyl compounds with docking studies
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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Senthamizh Selvan N., Agalya R., Maruthamuthu, Shameela Rajam, Christina Ruby Stella P.
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Full text available for: Characterization and antimicrobial activity of newly synthesized benzimidazolyl compounds with docking studies
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study reported in this paper focuses on the synthesis and characterization of newly synthesized benzimidazole derivatives, alongside their antimicrobial evaluation and docking studies. Benzimidazole is a prominent heterocyclic compound known for its widespread biological activities, which include applications in pharmaceuticals and agrochemicals. The objective of the research was to develop novel benzimidazole compounds with enhanced antimicrobial properties, targeting specific pathogens such as Staphylococcus aureus and Aspergillus niger.
Synthesis and Characterization of Benzimidazole Derivatives
The synthesis of two significant compounds, 2-(1H-benzo[d]imidazol-2-yl)-benzylidene amine and 2-[2-(1H-benzimidazol-2-yl)-phenylimino]-methyl phenol, was accomplished through a condensation reaction involving benzene-1,2-diamine and 2-aminobenzoic acid. The synthesized derivatives were thoroughly characterized using IR spectroscopy, 1H-NMR, and 13C-NMR, confirming the expected chemical structures. Notably, the compounds showcased characteristic absorption bands that corresponded to their functional groups, thus validating the successful synthesis.
Antimicrobial Activity Assessment
To evaluate the antimicrobial efficacy of the synthesized compounds, a disc diffusion method was implemented against the tested microorganisms, Staphylococcus aureus and Aspergillus niger. The results were promising, with the compound 2-(1H-benzo[d]imidazol-2-yl)-benzylidene amine exhibiting a significant zone of inhibition compared to control samples. Specifically, it demonstrated a superior antimicrobial activity against Staphylococcus aureus with a measurement of 22 mm, establishing it as a potential candidate for future antibiotic development.
Docking Studies and Binding Interaction
Molecular docking studies were performed to investigate the binding interactions of the synthesized compounds with the target protein COX2. The docking analysis focused on evaluating how well the compounds could fit into the binding site, specifically assessing their energy profiles. The compound A1, for example, achieved a binding energy of -73.88, suggesting a strong interaction with the target protein. Significant interaction residues were identified, including His 21, Ala54, Ser55, and Tyr65, indicating the potential of these synthesized compounds in therapeutic applications by effectively inhibiting the cyclooxygenase enzymes linked to inflammation.
Conclusion
The findings of this research highlight the successful synthesis and characterization of novel benzimidazole derivatives, demonstrating their potential antimicrobial activities and interactions with biological targets through molecular docking studies. The compound 2-(1H-benzo[d]imidazol-2-yl)-benzylidene amine, in particular, shows promise as a candidate for further pharmacological exploration. The study lays a foundational framework for future investigations aimed at developing effective pharmaceutical agents derived from benzimidazole compounds, with a need for continued research toward their therapeutic applications.
FAQ section (important questions/answers):
What compounds were synthesized for antimicrobial activity in this study?
The study synthesized two compounds: 2-(1H-benzo[d]imidazol-2-yl)-phenyl]-benzylidene amine and 2-[2-(1H-benzimidazol-2-yl)-phenylimino]-methyl phenol to evaluate their antimicrobial activity.
What techniques were used for characterizing the synthesized compounds?
The synthesized compounds were characterized using IR spectroscopy, 1H-NMR, 13C-NMR, and elemental analysis to confirm their structures and properties.
Which microorganisms were tested for antimicrobial activity of the compounds?
The compounds were screened for antimicrobial activity against Staphylococcus aureus and Aspergillus niger, comparing their effectiveness to reference standard drugs.
What were the results of the antimicrobial activity tests?
The compound 2-(1H-benzo[d]imidazol-2-yl)-phenyl]-benzylidene amine showed the highest antimicrobial activity, with inhibition zones of 22 mm for Staphylococcus aureus and 18 mm for Aspergillus niger.
What was the docking study performed on in this research?
Docking studies were conducted using DICLOFENAC bound to COX2 to assess the binding preferences of the synthesized compounds with the target protein.
What can be concluded about the synthesized compounds' potential?
The synthesized compounds exhibited moderate antimicrobial activity and the compound 2-(1H-benzo[d]imidazol-2-yl)-phenyl]-benzylidene amine showed significant potential for further drug development in treating inflammation.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Characterization and antimicrobial activity of new benzimidazoles.”. 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 study, 'activity' refers to the biological impact or effect of the synthesized compounds on specific microorganisms. This includes their antimicrobial effects against pathogens like Staphylococcus aureus and Aspergillus niger, indicating the effectiveness of the compounds in inhibiting microbial growth.
2) Pose:
'Pose' relates to the orientation and spatial arrangement of molecules during the docking studies. It represents how the synthesized compounds fit into the active site of the target protein COX-2, impacting their potential biological activity and efficacy as therapeutics.
3) Water:
In the synthesis methods described, water serves as a solvent and a medium for the precipitation and purification of synthesized compounds. It is crucial for creating a suitable reaction environment and for washing the products, ensuring the removal of impurities and enhancing the quality of the final compounds.
4) Drug:
The compounds synthesized in the research are evaluated for their potential as new drugs. 'Drug' signifies any chemical substance used in the diagnosis, treatment, or prevention of disease, with the focus here on their antimicrobial properties, particularly against resistant strains of bacteria.
5) Aureus:
This term references Staphylococcus aureus, a significant bacterial pathogen studied in this research for its response to the synthesized compounds. It is known for its resistance to antibiotics, making the development of new antimicrobial agents particularly relevant in combating infections caused by this bacterium.
6) Table:
In this manuscript, 'table' refers to a structured format that presents scientific data clearly. For example, a table summarizes the antimicrobial activity results, showing the zone of inhibition for the synthesized compounds compared to standard drugs, thereby facilitating easy interpretation of experimental findings.
7) Study (Studying):
The word 'study' indicates a systematic investigation aimed at discovering new methods or compounds. In this context, it encompasses the entire research process, including the synthesis, characterization of benzimidazole derivatives, and their evaluation for antibacterial properties, contributing to scientific knowledge in medicinal chemistry.
8) Discussion:
'Discussion' is a critical section of the research paper where results are interpreted, contextualized, and linked to existing literature. This part allows the authors to elaborate on their findings, explain the significance of the data, and propose future research directions or applications of the synthesized compounds.
9) Tamilnadu (Tamil-nadu):
Tamilnadu is a state in southern India, where the research was conducted. It provides geographical context for the study, highlighting the regional focus of scientific research activities within educational and research institutions in India, particularly at Bishop Heber College in Tiruchirapalli.
10) Medium:
'Medium' refers to the substances or environments used during the synthesis and testing of the compounds. In microbiological studies, it typically pertains to the nutrient agar or sabouraud dextrose agar used for culturing microorganisms, which is essential for assessing antibacterial efficacy.
11) Celvan:
Senthamizh Selvan N. is one of the authors of the study and thus is recognized for contributions to this research. Including the author's name acknowledges their role and expertise in the synthesis and evaluation of the b enzimidazole compounds, underscoring their involvement in scientific advancement.
12) India:
India, the country where the research was carried out, plays an essential role in the context of global pharmaceutical development. The scientific advancements and research outputs from India, particularly in medicinal chemistry and drug development, contribute to addressing local and global health challenges.
13) Pune:
Pune is a city in India where the microbial strains used in the study were obtained. It emphasizes the collaboration between different research institutions across India, showcasing how regional resources are leveraged for scientific research and the development of potential antimicrobial agents.
14) Life:
In this context, 'life' encompasses the biological processes and health aspects targeted by the synthesized compounds. The study ultimately aims to improve human health and quality of life by providing new therapeutic options against infections caused by pathogenic microorganisms.
15) Antibiotic (Antibacterial):
'Antibacterial' describes the property of a substance to inhibit the growth or kill bacteria. This term is central to the study as it defines the expected outcomes of the newly synthesized compounds, contributing to the quest for effective treatments against antibiotic-resistant bacterial infections.
16) Purification:
'Purification' refers to the process of isolating and refining the synthesized compounds to achieve a high degree of purity. It is a critical step in ensuring that the results of the antimicrobial activity tests are accurate and that the compounds are suitable for further analysis.
17) Inflammation:
Inflammation is a biological response to harmful stimuli, and the synthesized compounds are considered for their potential role in treating inflammation-associated conditions. This adds a layer of therapeutic application for the compounds beyond their antimicrobial properties, targeting broader health issues.
18) Quality:
'Quality' relates to the standard of the synthesized compounds and their effectiveness in therapeutic applications. Ensuring high-quality compounds is crucial for their reliability in antimicrobial activity and potential use in drug formulation, impacting overall medical outcomes.
19) Cancer:
Cancer refers to a group of diseases characterized by uncontrolled cell growth. The research hints at the link between the synthesized compounds and their effects on pathways involved in cancer biology, broadening their therapeutic implications beyond simple antimicrobial uses.
20) Nature:
In this study, 'nature' reflects the innate characteristics and behaviors of the synthesized compounds. Understanding the chemical nature of these compounds is pivotal in predicting their interactions with biological systems and their overall effectiveness as potential drugs.
21) Post:
'Post' relates to the post-docking analysis conducted to assess the interactions and binding energy of the synthesized compounds with the target protein. This evaluation step is crucial for understanding how well the compounds might perform in a biological context.
22) Ruby:
Christina Ruby Stella P. is another contributing author, highlighted to acknowledge her collaborative role in the research. Including her name signifies the collective effort in advancing knowledge in synthesizing and evaluating new antimicrobial compounds, reflecting teamwork in scientific inquiry.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Characterization and antimicrobial activity of new benzimidazoles.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Antimicrobial activity, Staphylococcus aureus, Aspergillus niger, Energy value, Docking studies, Spectroscopic analysis, Target Protein, Molecular docking study, Polyphosphoric acid.