Antimicrobial evaluation of substituted-benzoyl hydrazino pyrimidines.
Journal name: World Journal of Pharmaceutical Research
Original article title: Synthesis and antimicrobial evaluation of some substituted-benzoyl hydrazino derivatives of pyrimidine
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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Darshitkumar M. Dave and Dr. A. H. Bapodra
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synthesis and antimicrobial evaluation of some substituted-benzoyl hydrazino derivatives of pyrimidine
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20187-11689
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
Pyrimidines are a significant class of heterocyclic compounds widely utilized in drug discovery due to their extensive pharmacological activities. This research focuses on synthesizing aryl amide derivatives from pyrimidines, particularly substituted-benzoyl hydrazino derivatives. The newly synthesized compounds were characterized using infrared (IR) and nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry, and thin layer chromatography (TLC) to confirm their purity. Antimicrobial evaluations against various bacterial and fungal strains were carried out, evaluating their effectiveness in comparison to standard drugs.
Synthesis of Substituted-Benzoyl Hydrazino Derivatives
The synthesis of substituted-benzoyl hydrazino derivatives of pyrimidine was conducted through a multi-step procedure. Initially, methyl-4-(4-fluorophenyl)-2-hydrazinyl-6-isopropylpyrimidine-5-carboxylate was synthesized using POCl₃ and hydrazine hydrate. Subsequently, the main reaction involved the coupling of this intermediate with various substituted benzoyl chlorides in pyridine, resulting in the formation of different arylamide compounds (KLB a-j). This innovative synthesis route highlights the potential for creating structurally diverse derivatives through proper modification of the starting materials, which may lead to improved pharmacological profiles.
Antibacterial Activity Evaluation
The antibacterial properties of the synthesized compounds (KLB a-j) were assessed against several gram-positive and gram-negative bacteria. The results indicated that compound KLB g, containing a 3-CH₃ substituent, exhibited outstanding activity against Bacillus subtilis, outperforming the standard antibiotic ampicillin. Moreover, KLB j demonstrated significant effectiveness against Staphylococcus aureus. The compounds exhibited generally superior activity against gram-negative bacteria compared to gram-positive bacteria, showcasing the potential for optimizing the antimicrobial effects of pyrimidine derivatives through careful structural modifications.
Antifungal Activity Analysis
In addition to antibacterial evaluation, antifungal activity was tested against two fungal strains, Aspergillus niger and Aspergillus flavus. Among the synthesized derivatives, KLB g and KLB h (4-NO₂-C₆H₄) showed excellent antifungal effects against Aspergillus niger when compared to the standard drug nystatin. The compounds displayed varying levels of efficacy, suggesting that chemical modifications can lead to improved antifungal agents. Notably, KLB f and KLB g also exhibited significant activity against Aspergillus flavus, reinforcing the importance of functional group substitution in enhancing antifungal properties.
Conclusion
The current study successfully outlines an effective synthetic route for producing novel substituted-benzoyl hydrazino derivatives of pyrimidine, demonstrating significant antimicrobial activities. The evaluation of these compounds reveals their potential as effective antibacterial and antifungal agents, emphasizing the importance of further structural optimization in drug development. Future research should focus on exploring additional modifications to enhance efficiency and potency, potentially leading to therapeutically viable products against resistant microbial strains. The collaboration and support from various academic institutions further strengthened the exploration of these pharmacologically active compounds.
FAQ section (important questions/answers):
What are the biological activities of pyrimidine derivatives discussed?
Pyrimidine derivatives exhibit various biological activities, including anticonvulsant, antibacterial, and antifungal properties, making them significant in drug discovery.
How were the synthesized compounds characterized in this study?
The synthesized compounds were characterized using I.R. spectroscopy, NMR spectroscopy, mass spectrometry, and their purity was checked using Thin Layer Chromatography (TLC).
What method was used to test antimicrobial activity?
Antimicrobial activity was assessed using the microtitre broth dilution method and measuring the zone of inhibition against various bacterial and fungal strains.
Which compound showed the best antibacterial activity against specific bacteria?
Compound KLB g exhibited excellent antibacterial activity against Bacillus subtilis and KLB j showed maximum activity against Staphylococcus aureus compared to standard drugs.
How effective were the compounds against fungal strains?
The synthesized compounds displayed significant antifungal activity, particularly against Aspergillus niger, with KLB g and KLB h showing the most promising results.
What is the significance of the amide functionality in pharmaceuticals?
The amide functionality is common in many drugs, appearing in over 25% of known molecules, indicating its importance in enhancing pharmacological properties.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Antimicrobial evaluation of substituted-benzoyl hydrazino pyrimidines.”. 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 study, 'activity' refers to the biological effectiveness of the synthesized pyrimidine derivatives against various microbial strains. The research evaluates their antimicrobial properties through in vitro tests, measuring their capability to inhibit the growth of bacteria and fungi, thereby identifying potential therapeutic agents.
2) Drug:
Drugs represent a category of compounds with therapeutic potential. This study specifically refers to the development of new drugs derived from pyrimidine derivatives, emphasizing the importance of drug discovery in addressing infectious diseases through novel antimicrobial agents with improved efficacy and reduced resistance.
3) Antibiotic (Antibacterial):
The term 'antibacterial' describes compounds or activities that combat bacterial infections. The study focuses on the antibacterial properties of synthesized pyrimidine derivatives, assessing their efficacy against specific strains like Staphylococcus aureus and Escherichia coli, thereby establishing their potential role in fighting bacterial diseases.
4) Water:
Water in the experimental context refers to its role as a solvent or medium during chemical reactions and washing steps for the synthesized compounds. Proper handling and management of water are integral to ensuring purity and consistency in laboratory experiments, which is essential for reliable results.
5) Science (Scientific):
Science is fundamental to the research as it encompasses systematic exploration and experimentation to understand the pharmacological potential of chemical compounds. The study applies scientific methods in synthesis, analysis, and evaluation of new antimicrobial agents, contributing to the broader field of pharmaceutical chemistry and drug development.
6) Pharmacological:
Pharmacological relates to the study of drugs and their interactions in biological systems. This research emphasizes the pharmacological activities of pyrimidine derivatives, including their potential use to treat infections, underscoring the importance of pharmacological evaluation in identifying drugs that can efficiently target specific pathogens.
7) Gujarat:
Gujarat is the Indian state where the research was conducted. The geographical and cultural context can influence the focus of scientific research in the region, including local health challenges. This study highlights the scientific efforts in Gujarat aimed at addressing medicinal needs through innovative compound synthesis.
8) Aureus:
Staphylococcus aureus is a common bacterium and a target in the antimicrobial efficacy evaluation of the synthesized compounds. Its significance lies in its role as a pathogen responsible for a range of infections, making it a critical strain for testing the antibacterial effectiveness of new drug candidates.
9) India:
India, as the nation where this research was conducted, provides a diverse setting for antibiotic research due to its high burden of infectious diseases. The study aligns with India's goals in advancing healthcare and developing new therapeutic agents, thereby contributing to global health initiatives.
10) Table:
In the study, 'table' refers to organized data presentation containing the physical and antimicrobial activity results of the synthesized compounds. Tables are critical in scientific literature as they facilitate the clear communication of complex data, allowing for easier comparison and interpretation of experimental findings.
11) Purity:
Purity is a critical parameter for assessing the quality of synthesized compounds. In this research, the purity of the pyrimidine derivatives was evaluated through Thin Layer Chromatography (TLC). Ensuring high purity is essential for reliable antibacterial and antifungal testing, impacting the validity of the results.
12) Shri (Sr, Sri):
Shree is an honorific prefix used in Indian culture, often denoting respect and reverence. In the context of this study, it reflects the names of institutions and individuals involved in the research, highlighting the collaborative nature of academic endeavors in scientific inquiry.
13) Saurashtra (Saurastra):
Saurashtra is a region in Gujarat, India, where notable academic and scientific contributions take place. Mentioning Saurashtra affiliates the research with local educational institutions, underlining the significance of regional support in advancing scientific research and collaborative efforts in developing new pharmaceutical compounds.
14) Discussion:
Discussion in scientific research refers to the section that interprets and analyzes experimental results. This part of the article critically evaluates the antibacterial and antifungal activities observed in synthesized compounds, integrating findings with existing knowledge to draw conclusions and suggest further research directions.
15) Junagadh:
Junagadh is a city in Gujarat, India, significant for its educational institutions. Its mention in the study indicates the community's engagement in scientific research and the geographical context within which this research was conducted, highlighting academic contributions from this region.
16) Bhakta:
In the context of this research, Bhakta refers to Bhakta Kavi Narsinh Mehta University, which plays a role in conducting scientific research like the current study. This affiliation denotes the institutional support and resources that contribute to the success of the investigation in pharmacology.
17) Nature:
Nature describes the inherent characteristics or the biological significance of components being studied. This research captures the relationship between chemical structures and their biological activities, emphasizing how nature's diversity inspires the synthesis of new compounds for potential medicinal applications.
18) Study (Studying):
Study signifies the systematic investigation into the synthesis and activity of pyrimidine derivatives. This term encapsulates the research objectives, methodologies, and outcomes, reflecting the overall aim of contributing knowledge to the field of pharmaceutical chemistry and exploring new avenues in drug design.
19) Kavi:
Kavi, meaning poet in Hindi, forms part of the name Bhakta Kavi Narsinh Mehta University. Its inclusion reflects cultural aspects within the context of the research and highlights the importance of local heritage and pride in the academic community associated with the study.
20) Hand:
In this context, 'hand' refers figuratively to the assistance or involvement of individuals and institutions in the research process. It emphasizes collaborative efforts in scientific endeavors, showcasing how various contributors come together to achieve a common goal in drug discovery.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Antimicrobial evaluation of substituted-benzoyl hydrazino pyrimidines.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Pharmacological activities, Research article, Antimicrobial activity, Antifungal activity, Mass spectrometry, Standard drug, Gram positive bacteria, Gram negative bacteria, Thin Layer Chromatography (TLC), Minimum inhibitory concentration (MIC), Fungal strain, Biological activities, Pharmaceutical Research.