Synthesis and activity of benzoxazole-derived hydrazine carbothioamides
Journal name: World Journal of Pharmaceutical Research
Original article title: Synthesis, antiinflammatory and antioxidant activity of n-(benzoxazol-2-yl)-2-(2-oxoindolin-3- ylidine)hydrazine carbothioamides
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Arunadevi Parlapalli, Raparthi Vijay Kumar, Manasa Cidda and Sarangapani Manda
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synthesis, antiinflammatory and antioxidant activity of n-(benzoxazol-2-yl)-2-(2-oxoindolin-3- ylidine)hydrazine carbothioamides
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201714-9728
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The study detailed in this article focuses on the synthesis and evaluation of a series of new compounds known as N-(Benzoxazol-2-yl)-2-(2-oxoindolin-3-ylidine) hydrazine carbothioamides. Drawing on the biological significance of benzoxazole derivatives and isatin compounds, researchers synthesized a total of seven new derivatives and tested them for their anti-inflammatory and antioxidant activities. The research highlights the promising potential these synthesized compounds have in pharmacological applications.
Synthesis and Characterization of New Compounds
The synthesis of N-(Benzoxazol-2-yl)-2-(2-oxoindolin-3-ylidine) hydrazine carbothioamides involved multiple steps, including the creation of intermediates like 2-amino benzoxazole and isatin from isonitrosoacetanilides. Characterization techniques such as melting point determination, infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry confirmed the identity and purity of the synthesized compounds. The results indicated successful synthesis with varying yields, melting points, and molecular weights among the derivatives.
Antiinflammatory Activity Evaluation
The anti-inflammatory potential of the synthesized compounds was assessed using a modified carrageenan-induced paw edema model in Wistar strain albino rats. Among the test compounds, Vc (R=5-NO2), Vd (R=5-Br), and Va (R=5-H) exhibited significant reductions in inflammation compared to the standard drug indomethacin. The compounds were evaluated for their efficacy in reducing paw edema at multiple time intervals, with the most effective displaying up to a 61.1% inhibition of edema after four hours.
Antioxidant Activity Assessment
The antioxidant activity of the synthesized compounds was measured using the DPPH (2,2-diphenyl-1-picrylhydrazyl) method. This assessment provided insight into the scavenging ability of these compounds against free radicals. The compounds Va (R=5-H) and Ve (R=5-CH3) demonstrated notable antioxidant activity with IC50 values of 30.71 µM and 50.43 µM, respectively. Other derivatives showed varying degrees of antioxidant effects, indicating that structural modifications significantly influenced their activities.
Conclusion
The study concluded that the newly synthesized N-(Benzoxazol-2-yl)-2-(2-oxoindolin-3-ylidine) hydrazine carbothioamides possess promising anti-inflammatory and antioxidant properties. Compounds Vc, Vd, and Va emerged as the most potent candidates in the anti-inflammatory evaluation, while Va and Ve showed marked antioxidant potential. These findings suggest that further exploration of these compounds may lead to the development of new pharmaceutical agents for combating inflammation and oxidative stress-related conditions.
FAQ section (important questions/answers):
What compounds were synthesized in Arunadevi Parlapalli's study?
A series of seven new compounds, specifically N-(Benzoxazol-2-yl)-2-(2-oxoindolin-3-ylidine)hydrazine carbothioamides, were synthesized using different isatins and N-(Benzoxazol-2-yl)hydrazine carbothioamide.
What was evaluated for anti-inflammatory activity in the study?
The anti-inflammatory activity of the test compounds was evaluated using a carrageenan-induced paw edema model in Wistar albino rats, comparing the results to the standard drug indomethacin.
Which compounds showed the most promising anti-inflammatory activity?
Compounds Vc (R=5-NO2), Vd (R=5-Br), and Va (R=5-H) significantly reduced inflammation and showed promising anti-inflammatory activity.
What method was used to test antioxidant activity?
The antioxidant activity of the compounds was evaluated via the DPPH method, measuring the concentration of the compound needed to scavenge 50% of free radicals.
Which compounds exhibited the highest antioxidant activity?
Compounds Va (R=5-H) and Ve (R=5-CH3) exhibited the highest antioxidant activity among the tested compounds.
What biological activities are associated with benzoxazole derivatives?
Benzoxazole derivatives are known for various biological activities, including anticancer, antimicrobial, and anti-inflammatory properties.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Synthesis and activity of benzoxazole-derived hydrazine carbothioamides”. 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' in the context of this study refers to the biological effects exhibited by the synthesized compounds, specifically their anti-inflammatory and antioxidant activities. These activities are crucial for determining the therapeutic potential of the compounds in treating inflammation and oxidative stress-related disorders, thereby guiding further research and development.
2) Edema (Oedema):
Edema refers to the swelling caused by excess fluid accumulation in tissues, often used as a clinical feature in studies assessing anti-inflammatory agents. In this research, paw edema was induced in rats using carrageenan to evaluate the anti-inflammatory effects of new compounds, serving as a model for inflammatory responses.
3) Water:
Water serves as a solvent in various chemical reactions and preparation methods outlined in the study. It is often utilized for dissolving reactants or washing products, demonstrating its fundamental role in experimental protocols. The study incorporates water in the synthesis of isatin and related compounds, highlighting its importance in pharmaceutical chemistry.
4) Inflammation:
Inflammation is a biological response to harmful stimuli, including pathogens or injuries, characterized by redness, heat, swelling, and pain. This study investigates the anti-inflammatory properties of synthesized compounds, which seeks to establish their efficacy in moderating the inflammatory response, thereby offering potential therapeutic benefits in inflammatory diseases.
5) Table:
In scientific literature, 'Table' often denotes structured data presenting experimental results, such as the anti-inflammatory effects of compounds or their antioxidant activities. The tables within the study provide clear, comparative summaries of data, allowing for easy assessment of each compound's performance relative to standards and across different tests.
6) Animal:
The term 'Animal' pertains to the use of Wistar albino rats in this study, serving as a model organism for testing the biological activity of new compounds. Animal testing is essential in preclinical studies to evaluate safety, efficacy, and pharmacodynamic properties before progressing to human trials, thus highlighting ethical considerations.
7) Drug:
In the context of this research, 'Drug' refers to the synthetic compounds being tested for medicinal properties. The compounds' potential to act as therapeutic agents demonstrates the ongoing search for new drugs within pharmacology to address inflammation and oxidative damage, contributing to advancements in drug development.
8) Pharmacological:
The term 'Pharmacological' relates to the study of the interactions between drugs and biological systems. The research focuses on evaluating the pharmacological properties of synthesized N-(Benzoxazol-2-yl)-2-(2-oxoindolin-3-ylidine) hydrazine carbothioamides, shedding light on their therapeutic potential and mechanisms of action against inflammation and oxidative stress.
9) Kakatiya:
Kakatiya refers to Kakatiya University, the institution where the research was conducted. The university's affiliation underscores its commitment to academic and scientific research, fostering innovation in pharmaceutical sciences. This connection enhances the credibility of the findings and represents institutional support for advancements in health sciences.
10) Warangal:
Warangal is a city in India where Kakatiya University is located. By mentioning 'Warangal,' the study highlights the geographical context of the research, which can influence local academic collaborations and public health efforts. It also reflects the regional support for scientific inquiry into pharmaceutical advancements.
11) Science (Scientific):
Science in this context refers to the systematic study of the natural world, including the research processes, methodologies, and analytical techniques employed in synthesizing and testing the new compounds. The scientific approach ensures the findings are valid, reproducible, and contribute to the body of knowledge in pharmaceutical research.
12) Hind:
Hind, likely referring to 'Hindu' or 'Hindustan,' could imply cultural relevance or the geographical context of the study. It may also suggest the need for culturally appropriate healthcare solutions, particularly in pharmacology and drug development, addressing health issues pertinent to the local population being studied.
13) Antibiotic (Antibacterial):
Antibiotic refers to substances that can kill or inhibit the growth of bacteria, relevant in the context of evaluating biological activities of the synthesized compounds. Although the focus here is on anti-inflammatory and antioxidant properties, antibiotic potential previously found in benzoxazole derivatives could warrant further investigation in pharmacological settings.
14) Discussion:
Discussion sections in research articles evaluate results, interpret data, and compare findings with existing literature. It allows authors to elaborate on the implications of their findings, addressing any limitations and proposing future research directions. Hence, the discussion in this study contextualizes the significance of anti-inflammatory and antioxidant activities observed.
15) Heating:
Heating is a crucial process in chemical synthesis, as it can drive reactions forward and influence the formation of desired products. In this study, heating is utilized during the synthesis of isatin, demonstrating its importance in achieving necessary temperature conditions for optimal reactions in pharmacological compound development.
16) Manasa (Manasha):
Manasa refers to one of the co-authors involved in the research. Citing researchers' names acknowledges their contributions and collaboration in the study, emphasizing the importance of teamwork in scientific efforts. It also showcases the individuals behind the findings and promotes recognition of academic and research impact.
17) Purity:
Purity indicates the degree to which a compound is free from contamination or impurities, crucial in drug development. The study mentions checks for purity using Thin Layer Chromatography (TLC), which is vital to ensure the reliability and consistency of results, promoting safety and efficacy in potential pharmaceutical applications.
18) Manda (Mamda):
Manda refers to another co-author of the research. Including authors' names acknowledges their contributions and enhances accountability in scientific reporting. This recognition fosters a collaborative environment within academia, underlining the importance of collective efforts in advancing knowledge and drug research in the pharmaceutical sciences.
19) Kumar:
Kumar denotes a co-author of the study. Mentioning authors serves not just to credit their work but also to emphasize the collaborative nature of scientific research. It highlights the contributions of each researcher in the synthesis, testing, and analysis of new pharmaceutical compounds for their medicinal activities.
20) Pur:
Poor in a scientific context often describes inadequate performance or low activity levels, as seen in the discussion of antioxidant efficacy measured by IC50 values. This term serves to categorize the tested compounds, providing a comparative basis for evaluating the effectiveness of the synthesized compounds against established standards in pharmacological performance.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Synthesis and activity of benzoxazole-derived hydrazine carbothioamides’. Further sources in the context of Science might help you critically compare this page with similair documents:
Anti-inflammatory activity, Antioxidant activity, Rat model, Pharmacological action, Thin Layer Chromatography (TLC), Carrageenan-induced paw edema, IC50 value, Mass spectrum, 1H NMR spectra, Biologically active compound, Standard drug indomethacin, Ethanol reflux.