"New 3-(2-(2-phenyl-1H-benzimidazol-1-yl)acetyl)-2H-chromen-2-one"
Journal name: World Journal of Pharmaceutical Research
Original article title: New 3-(2-(2-phenyl-1h-benzo [d] imidazol-1-yl) acetyl)-2hchromen- 2-one analogues as potential antimicrobial agents
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Shailesh S. Gurav and Krishnakant T. Waghmode
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: New 3-(2-(2-phenyl-1h-benzo [d] imidazol-1-yl) acetyl)-2hchromen- 2-one analogues as potential antimicrobial agents
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr202013-18987
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The study presented in the article explores the synthesis and antibacterial properties of new 3-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)acetyl)-2H-chromen-2-one analogues. Conducted by Shailesh S. Gurav and Krishnakant T. Waghmode from the Department of Chemistry at D. G. Ruparel College, this research focuses on the derivatives of benzimidazole and coumarin due to their notable biological activities. The synthesis process involves several chemical reactions, including the formation of 3-acetyl coumarin and the subsequent creation of benzimidazole derivatives, leading to the synthesis of compounds that exhibit potential antimicrobial properties.
Importance of Benzimidazole Derivatives
Benzimidazole derivatives are recognized for their diverse biological activities, which encompass antibacterial, antifungal, analgesic, and anticancer properties, among others. The article highlights their significance as privileged structures in new pharmaceutical developments. The synthesized benzimidazole compounds in this study were created through N-alkylation reactions, indicating their versatility in chemical modifications to enhance bioactivity. Additionally, these compounds have shown important interactions with various biochemical targets, making them significant candidates for further pharmacological exploration.
Antibacterial Evaluation
The antibacterial activity of the synthesized compounds was rigorously evaluated against four pathogenic bacterial strains, including both Gram-positive and Gram-negative bacteria. The compounds exhibited varied levels of antimicrobial effectiveness, with some showing promising results comparable to the standard antibiotic erythromycin. Specifically, compounds 4a and 4d demonstrated the most substantial activity against Staphylococcus aureus, while compounds 4a and 4e showed strong effectiveness against Escherichia coli. This suggests the potential application of these new benzimidazole derivatives as therapeutic agents in combating bacterial infections.
Computational Studies and Drug-Likeness
Alongside the experimental evaluations, the article employed computational tools to screen the most active compound, 4a. It highlighted promising pharmacokinetic properties and a high likelihood of interaction with various biological targets, particularly kinases. The drug-likeness analysis conducted using the Swiss ADME tool indicated compliance with the Lipinski rule of five, suggesting that compound 4a is a suitable candidate for further drug development. These computational predictions bolster the potential for the synthesized compounds to be explored as therapeutic agents in future studies.
Conclusion
The research successfully demonstrates that the newly synthesized coumarin-induced benzimidazole derivatives exhibit significant antimicrobial properties, establishing a foundation for further investigations into their pharmacological applications. The study emphasizes the importance of these compounds in the context of medicinal chemistry and their potential as effective agents against various pathogenic organisms. The combination of synthetic, biological, and computational approaches in this study underscores the multilayered process of drug discovery, suggesting that these compounds could become valuable in the fight against antibiotic resistance and other infectious diseases.
FAQ section (important questions/answers):
What compounds were synthesized in the study?
The study synthesized new 3-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)acetyl)-2H-chromen-2-one analogues, focusing on their antibacterial properties.
What are the key biological activities of benzimidazole derivatives?
Benzimidazole derivatives exhibit various activities, including antibacterial, antifungal, analgesic, antitumoral, and antiparasitic properties.
How were the synthesized compounds tested for antibacterial activity?
The compounds were screened against two Gram-positive and two Gram-negative bacteria using agar well diffusion and measuring the zone of inhibition.
What was the most active compound against the tested bacterial strains?
Compound 4a exhibited the highest antibacterial activity against Staphylococcus aureus and Escherichia coli.
What method was used for the synthesis of benzimidazole compounds?
Benzimidazole compounds were synthesized via N-alkylation of 2-substituted benzimidazole with 3-(2-bromoacetyl)-2H-chromen-2-one.
What does the Swiss Target Prediction indicate for compound 4a?
The Swiss Target Prediction suggests compound 4a is likely to act on kinases, indicating potential for anticancer activity.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “"New 3-(2-(2-phenyl-1H-benzimidazol-1-yl)acetyl)-2H-chromen-2-one"”. 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 rate or degree of something working effectively. In the context of this research article, it pertains to the antibacterial activity of the synthesized benzimidazole derivatives. Specific measurements, such as the zone of inhibition, gauge how well these compounds inhibit bacterial growth, indicating their potential as therapeutic agents.
2) Antibiotic (Antibacterial):
Antibacterial refers to substances that destroy or inhibit the growth of bacteria. In the study, the synthesized coumarin-induced benzimidazole derivatives are evaluated for their antibacterial properties against various strains of bacteria. These findings are crucial for developing new antibiotics to combat bacterial infections resistant to existing treatments.
3) Aureus:
Aureus is a species of bacteria, specifically Staphylococcus aureus, known for causing a range of infections. In the research study, the activity of the synthesized compounds is assessed against this bacterium, which serves as a significant target for antibacterial drug development due to its prevalence in clinical settings.
4) Water:
Water is a universal solvent and a key ingredient in many chemical reactions and syntheses in the laboratory. In this study, distilled water is utilized for various preparations and washing steps during the synthesis of chemical compounds, highlighting its essential role in the experimental procedures.
5) Study (Studying):
Study encompasses the systematic investigation into the activity and properties of synthesized compounds. In this research, the main focus is on the synthesis of new derivatives and their biological activity against bacteria, aiming to contribute to the field of medicinal chemistry and pharmacy through novel antibacterial agents.
6) Drug:
Drugs encompass a wide range of substances intended for use in the diagnosis, treatment, or prevention of diseases. In this study, the synthesized compounds are evaluated for their potential as new pharmaceutical agents. The focus on developing effective drugs highlights the importance of addressing antibiotic resistance in healthcare.
7) Table:
Table refers to a structured arrangement of data. In this research, tables are utilized to present experimental results, particularly the antibacterial activity data of synthesized compounds. By organizing this information, the authors allow for easy comparison and analysis of the efficacy of the different derivatives.
8) Maharashtra (Maharastra, Maha-rashtra):
Maharashtra is a state in India where the research was conducted. It is relevant as it provides the geographical and institutional context of the study. The local academic and research community, specifically at D. G. Ruparel College in Mahim, contributed resources and facilities for this scientific inquiry.
9) India:
India is the country where the research took place. Its relevance includes providing context for the research environment, as well as potential implications for public health. In a country facing diverse microbial challenges, effective new antimicrobial agents are especially important for combating infections prevalent in Indian healthcare settings.
10) Family:
Family can refer to a biological classification. In this context, it relates to categorizing compounds and their interactions, particularly in pharmacology. Understanding the family of compounds helps predict their behavior, interactions with biological targets, and potential side effects, which is essential for drug development.
11) Indian:
Indian pertains to being from India or relating to its culture and scientific practices. In the context of this research, it highlights the regional focus of the study, emphasizing the contributions of local scientists and the relevance of findings to public health challenges faced in India.
12) Discussion:
Discussion refers to the section where researchers interpret results and place them in the context of existing literature. In this paper, the discussion examines the significance of findings, compares them with previous work, and proposes future directions based on the antibacterial efficacy observed in the synthesized compounds.
13) Nature:
Nature often refers to the natural world or the inherent characteristics of substances. In this study, it highlights the biological properties and behaviors of the synthesized compounds, specifically their interactions with bacteria. Understanding the nature of these compounds is essential for assessing their potential therapeutic applications in medicine.
14) Medium:
Medium refers to the environment in which bacteria grow, in this case, a nutrient agar medium. The composition of this medium is crucial for properly cultivating bacteria during the experiments. The effectiveness of synthesized compounds is evaluated in the context of their ability to inhibit bacteria grown in this medium.
15) Saxena (Sakshena, Saksena):
Saxena is a surname likely representing one of the researchers or contributors mentioned in the references or acknowledgments of the study. The specific contributions of individuals like Saxena can reflect broader collaborative efforts in the scientific community that support research and development of new pharmaceutical agents.
16) Egypt:
Egypt is a country that may feature in the references, particularly regarding previous studies or research discussed in the paper. It highlights the global context of scientific research and its relevance across countries, linking findings in this study with broader international research efforts and advancements in medicinal chemistry.
17) Bordi:
Bordi, like Saxena, likely refers to one of the contributors to previous research mentioned in the article. Acknowledging various researchers helps demonstrate the collaborative nature of scientific inquiry and emphasizes the interconnectedness of findings within the global scientific community.
18) Sah:
Shah may refer to a researcher mentioned in the references or acknowledgments of the study. The mention of various authors, such as Shah, underscores the importance of collaborative research and past contributions that have influenced current findings and direction in the field of medicinal chemistry.
19) Food:
Food refers to substances consumed for nutritional support. Its relevance in this study may arise from the use of certain compounds as additives or preservatives. Additionally, compounds with antibacterial properties might have implications for food safety and preventing pathogens from contaminating food products in various contexts.
20) Kubo:
Kubo is likely a reference to a researcher or a specific study discussed within the article. Its mention highlights the importance of past research in shaping the current findings and suggests critical insights from various researchers that contribute to understanding the properties of synthesized compounds.
21) Hand:
Hand can refer to both a physical appendage and idiomatically the support given by others. In the context of scientific research, it can signify collaboration and teamwork in conducting experiments and interpreting data, where researchers depend on one another's expertise to achieve successful outcomes in their studies.
22) Qian:
Qian refers to another researcher whose work may be cited in the study. The inclusion of various authors emphasizes the collaborative nature of scientific research and acknowledges the contributions of multiple individuals to the advancement of knowledge and discovery in the field of medicinal chemistry.
Other Science Concepts:
Discover the significance of concepts within the article: ‘"New 3-(2-(2-phenyl-1H-benzimidazol-1-yl)acetyl)-2H-chromen-2-one"’. Further sources in the context of Science might help you critically compare this page with similair documents:
Zone of inhibition, Minimum inhibitory concentration, Antibacterial activities, Gram positive bacteria, Gram negative bacteria, Bioactivity, Spectral data, World Journal of Pharmaceutical Research, Department of Chemistry, Pharmaceutical properties, Pharmacokinetic profile, Coumarin Derivative, Swiss Target Prediction.