Green synthesis and antimicrobial assessment of novel thiazolidinones.
Journal name: World Journal of Pharmaceutical Research
Original article title: Facile green synthesis and antimicrobial evaluation of some novel thiazolidinones with pyrimidine moiety
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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Summary of article contents:
Introduction
The study conducted by Pravina Baburao Piste and Maruti Sidhu Kanase focuses on the green synthesis and antimicrobial evaluation of novel thiazolidinones incorporating pyrimidine moieties. Leveraging microwave irradiation technology, the researchers synthesized 6-methyl-4-(Substituted) Phenyl-2-Oxo/Thioxo-1,2,3,4-Tetrahydropyrimidine derivatives. These compounds underwent in vitro screening for their antimicrobial activities against Staphylococcus aureus and Escherichia coli, resulting in certain compounds exhibiting significant biological efficacy. This research underscores the potential of thiazolidinone derivatives as promising candidates in medicinal chemistry.
Microwave-Assisted Synthesis
The study highlights a crucial advancement in the synthesis process through the use of microwave irradiation, which presents significant advantages over conventional heating methods. This technology reduces reaction time from hours to mere minutes, enhances yields, and minimizes side reactions, making it environmentally friendly. The thiazolidinone core structure, which is at the heart of this research, is notable for its presence in various pharmaceuticals with a wide spectrum of biological activities. The authors developed an efficient, cost-effective, and eco-friendly protocol using microwave-assisted synthesis, demonstrating its practicality in producing biologically active compounds.
Antimicrobial Screening Results
An important outcome of the study was the screening of synthesized compounds for their antimicrobial activities, which was conducted using the disc diffusion method. The researchers evaluated the compounds against both Gram-positive (S. aureus) and Gram-negative (E. coli) bacteria. Notably, compounds IVg and IVh exhibited antibacterial activity levels comparable to the standard drug, streptomycin, particularly when electron-withdrawing substituents such as nitro groups were present. Other compounds displayed moderate antimicrobial activity, contributing valuable data to the understanding of structure-activity relationships in thiazolidinone derivatives.
Spectral Characterization and Analysis
The synthesized compounds were rigorously characterized using various analytical techniques, including Infrared (IR) spectroscopy, Proton Nuclear Magnetic Resonance (1H NMR), and Mass Spectrometry. These methodologies corroborated the chemical structures assigned to the compounds, affirming the successful formation of thiazolidinone derivatives. The researchers observed distinct spectral features that showcased the presence of functional groups, such as the disappearance of certain peaks during various reaction stages, indicating successful transformations. Elemental analysis further validated the molecular formulae, linking experimental results to theoretical expectations.
Conclusion
In conclusion, this research successfully demonstrates a microwave-assisted, environmentally benign method for synthesizing thiazolidinone derivatives with potential pharmacological applications. The study's findings indicate that certain compounds possess moderate to excellent antimicrobial activity, with some outperforming standard antibiotics. The results contribute to the ongoing exploration of thiazolidinones in medicinal chemistry, affirming their significance as versatile scaffolds for developing new therapeutic agents. The research also emphasizes the critical balance between innovative synthesis techniques and biological evaluation in advancing drug discovery.
Original source:
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Pravina Baburao Piste and Maruti Sidhu Kanase
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Facile green synthesis and antimicrobial evaluation of some novel thiazolidinones with pyrimidine moiety
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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FAQ section (important questions/answers):
What is the main focus of the research article by Pravina et al.?
The research article focuses on the facile green synthesis and antimicrobial evaluation of novel thiazolidinones containing a pyrimidine moiety, exploring their antibacterial activity against S. aureus and E. coli.
What method was used for synthesizing the compounds in the study?
The compounds were synthesized using microwave (MW) irradiation, which provided a reduced reaction time and improved yields compared to conventional heating methods.
Which methods were used to characterize the synthesized compounds?
The synthesized compounds were characterized using IR spectroscopy, 1H NMR spectroscopy, mass spectrometry, and elemental analysis to confirm their structures and purity.
What were the results of the antimicrobial activity testing?
The antimicrobial activity of the synthesized compounds was evaluated using the disc diffusion method, revealing variable activity, with some compounds showing significant effects against both Gram-positive and Gram-negative bacteria.
How did the presence of electron-withdrawing groups affect activity?
Compounds with electron-withdrawing groups, specifically nitro substituents, exhibited enhanced antimicrobial activity compared to other derivatives, indicating their potential role in improving biological activity.
What conclusions were drawn from the research findings?
The study concluded that the synthesized thiazolidinone derivatives displayed moderate to excellent antimicrobial activity, with some compounds showing results comparable or superior to the standard antimicrobial drug, streptomycin.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Green synthesis and antimicrobial assessment of novel thiazolidinones.”. 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 the article, 'Activity' refers specifically to the biological activity of the compounds that were synthesized and evaluated, particularly their antimicrobial effects against bacteria. The article highlights the importance of this activity in assessing the potential medicinal value of the synthesized thiazolidine derivatives against pathogens like S. aureus and E. coli.
2) Shatara (Satara, Śatāra, Śaṭara):
Satara is noteworthy as it is the location of the institutions involved in the research detailed in the article. It reflects the geographical and cultural context where scientific advancements are being pursued, providing insight into the local contributions to the field of medicinal chemistry in India.
3) Drug:
'Drug' in this text pertains to the potential medications developed from the novel thiazolidine-4-one derivatives. The mention of drugs underscores the research aim of discovering new medicinal compounds that could treat infections, thus highlighting the relevance of this study within pharmaceutical development.
4) Aureus:
The term 'Aureus' refers to Staphylococcus aureus, a common bacterium responsible for various infections. Its mention underscores the focus of the antimicrobial evaluation in the study, as the synthesized compounds were tested specifically against this pathogen, highlighting their potential application in combatting bacterial infections.
5) India:
India is significant as it provides the socio-cultural and institutional framework within which the research was conducted. The context of scientific research in India, particularly in medicinal chemistry, is essential to understanding the progress and challenges faced in developing new pharmaceutical compounds.
6) Antibiotic (Antibacterial):
The term 'Antibacterial' relates to the specific activity of the synthesized compounds to inhibit the growth of bacteria, particularly against Gram-positive and Gram-negative strains. This property is crucial for assessing their potential as therapeutic agents in treating bacterial infections, which is a central theme of the research.
7) Maharashtra (Mahārāṣṭra, Maha-rashtra):
Maharashtra is the Indian state where the associated institutions are located. Its mention contextualizes the research geographically, indicating the regional focus and involvement in the scientific community in India, particularly in the fields of chemistry and pharmaceutical research.
8) Science (Scientific):
The term 'Science' in the article emphasizes the systematic approach to understanding and applying scientific principles in the field of drug synthesis. It highlights the methods, analyses, and discussions employed to derive new compounds, reinforcing the importance of scientific rigor in medicinal chemistry.
9) Table:
The word 'Table' refers to the organized presentation of data within the study, specifically detailing the physical properties and antimicrobial activities of the synthesized compounds. Tables serve as a crucial visualization tool to convey complex information efficiently and are essential in scientific reporting.
10) Water:
Water is mentioned in the context of purification steps during the synthesis process. It signifies the role of simple laboratory processes in handling chemical reactions, emphasizing the practical aspects of chemistry experiments and the importance of solvents in obtaining pure compounds.
11) Discussion:
The section labeled 'Discussion' is where researchers interpret their findings, analyzing the results’ implications in the context of existing literature. It provides insights into the significance of the antimicrobial activities observed, contributing to a deeper understanding of the new compounds' potential applications.
12) Kolhapur (Kolhāpur):
Kolhapur is another locality in the state of Maharashtra that plays a role in this research, particularly in providing support for spectral interpretations. Mentioning Kolhapur situates the research within a wider collaborative scientific network, valuable for understanding regional contributions to medicinal chemistry.
13) Heating:
The term 'Heating' relates to the process used for the synthesis of the compounds, especially microwave irradiation, which serves as a modern technique for facilitating chemical reactions. Emphasizing heating underscores its role in improving efficiency in synthesis and reflects advancements in chemical methodologies.
14) Maruti (Māruti, Maṟuti):
Maruti Sidhu Kanase, the co-author mentioned in the text, plays a significant role in the research. Including personal names in the study highlights the collaborative nature of scientific research and acknowledges contributions of individuals in the development and exploration of new pharmaceutical compounds.
15) Purity:
Purity is a vital quality attribute in the synthesized compounds and pertains to the degree to which a chemical substance is free from impurities. In pharmaceutical research, high purity is essential for ensuring reliable biological testing and efficacy, cementing the significance of this factor in drug development.
16) Sidhu (Sīdhu, Shidhu, Śīdhu):
The name Sidhu refers to Maruti Sidhu Kanase, the co-author of the study, who contributed to the research on thiazolidine derivatives. Including authors' names establishes accountability, provides recognition for their work, and highlights the collaborative efforts in scientific inquiry and development.
17) Study (Studying):
The word 'Study' encapsulates the entire research undertaken, focusing on the synthesis, characterization, and biological evaluation of new compounds. It signifies a systematic investigation process aimed at contributing to the body of knowledge in medicinal chemistry and potential therapeutic applications.
18) Pur (Pūr):
'Poor' in the context of antimicrobial activity signifies the compounds that exhibited low effectiveness against the tested pathogens. This acknowledgment is crucial in scientific research as it emphasizes the variable nature of compound efficacy and frames future research directions to improve molecular activity.