Critical review on isoxazoles
Journal name: World Journal of Pharmaceutical Research
Original article title: Critical review on isoxazoles
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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A. Kanaka Raju,, Dr. Y. Srinivasa Rao and Dr. Ch. Prasad
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Critical review on isoxazoles
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201610-6994
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Summary of article contents:
Introduction
Isoxazoles, characterized by their five-membered heterocyclic ring containing nitrogen and oxygen, have garnered significant attention in pharmaceutical research for their potential therapeutic activities. Recent studies focus on the synthesis, characterization, and biological evaluation of various substituted isoxazoles, which are being explored as potential drugs for a range of pathological diseases. This review encapsulates the methodologies for preparing these compounds, their molecular characterization, and the biological activities that make them bioactive candidates in modern medicine.
Therapeutic Potential of 2-Isoxazolines
Substituted 2-isoxazolines have demonstrated a broad spectrum of biological activities, making them noteworthy in the realm of drug discovery. Various studies highlight their antimicrobial, anti-inflammatory, and anticancer properties, among others. The synthesis of these compounds often involves modifications to the core isoxazoline structure, resulting in analogs that exhibit enhanced activity. For instance, certain derivatives have shown significant antifungal activity against pathogens like Dreschslera tetramera and Fusarium oxysporum, while also presenting efficacy in combating bacterial strains such as Escherichia coli and Staphylococcus aureus. This diversity in biological activity showcases the potential of 2-isoxazolines as versatile therapeutic agents.
Synthesis Techniques and Mechanisms
The synthesis of isoxazolines typically employs a variety of methodologies, notably including the treatment of allylic esters and aldoximes. For example, allylic esters can be treated under specific conditions to yield 2-isoxazoline derivatives, while N-tert-butyl-N-chlorocyanamide can be utilized with aldoximes to produce hydroximoyl chlorides that subsequently lead to nitrile oxides and isoxazolines. A key aspect of these synthesis methods is their efficiency and the mild conditions under which they operate, allowing for high yields and the ability to explore structural modifications that enhance therapeutic potentials.
Significance of Isoxazoles in Drug Development
Isoxazoles play a crucial role in the development of novel drugs aimed at treating various medical conditions. Research has shown that derivatives of isoxazolines are being explored as candidates for treating thromboembolic disorders through their action as factor Xa inhibitors. Additionally, they have been investigated for their capacities in managing inflammation, serving as dual inhibitors against platelet aggregation, and showing potential in anticancer therapies. This ongoing exploration underscores the importance of isoxazoles in designing new therapeutics with improved efficacy and safety profiles.
Conclusion
In summary, the review emphasizes the promise of substituted isoxazolines in pharmaceutical research, showcasing their diverse biological activities and potential therapeutic applications. The ongoing synthesis and refinement of these compounds represent a significant area of focus within drug discovery, highlighting the need for continued research into their mechanisms and interactions. As the field progresses, isoxazoles are likely to remain central to the development of effective treatments for a variety of pathological conditions, reflecting their versatility and utility in modern medicine.
FAQ section (important questions/answers):
What are isoxazoles and their significance in pharmaceuticals?
Isoxazoles are five-membered heterocycles containing nitrogen and oxygen. They are significant due to their diverse biological activities, making them potential candidates for drug development against various diseases.
What biological activities are associated with substituted isoxazoles?
Substituted isoxazoles exhibit various biological activities including antimicrobial, anti-inflammatory, anticancer, and anti-HIV properties among others, making them valuable in pharmaceutical research.
How are isoxazolines synthesized in the laboratory?
Isoxazolines are synthesized through methods such as treatment of allylic esters and aldoximes, employing reagents like NOBF4 and N-tert-butyl-N-chlorocyanamide, resulting in different isoxazoline derivatives.
What is the therapeutic potential of 2-isoxazolines?
2-Isoxazolines show considerable potential as chemotherapeutic agents with activities such as inhibiting fibrinogen receptors and acting against various pathogens, including bacteria and fungi.
What are common applications of isoxazoline derivatives in medicine?
Isoxazoline derivatives have applications in treating infections, inflammatory conditions, and cancer. They also display activities against thrombotic and immunological disorders.
Can isoxazoles be used for drug development?
Yes, isoxazoles are promising candidates in drug development due to their wide range of bioactivities, which can be enhanced through structural modifications in their chemical design.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Critical review on isoxazoles”. 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 pharmacology, 'activity' refers to the capability of a compound or drug to produce a desired effect in biological systems. It can include therapeutic effects, such as antimicrobial or anti-inflammatory actions. The relevance of 'activity' is paramount in drug discovery, as researchers seek to identify compounds that exhibit significant biological responses in preclinical and clinical trials.
2) Antibiotic (Antibacterial):
'Anti-bacterial' is a term synonymous with antibacterial, indicating substances that target bacterial infections. This label is critical for drugs developed to treat infections caused by bacteria, promoting the importance of identifying new compounds with this activity to mitigate the growing issue of resistance in bacterial pathogens.
3) Disease:
'Disease' signifies a pathological condition characterized by specific signs and symptoms. The article identifies various diseases that are targeted by pharmacological interventions, emphasizing the importance of researching compounds that can combat these conditions, ranging from infections to chronic diseases, improving overall health outcomes.
4) Aureus:
'Aureus' refers to Staphylococcus aureus, a common bacteria that can cause serious infections in humans. The mention of 'aureus' highlights the need for effective treatments against resistant strains, underscoring ongoing research to develop antibacterial agents capable of controlling infections caused by this opportunistic pathogen.
5) Drug:
'Drug' is a broad term that refers to any substance used for medical treatment. In pharmaceutical research, identifying potential new drugs, understanding their mechanisms of action, and evaluating their efficacy and safety are critical aspects of developing effective therapies for various ailments and diseases.
6) Line:
'Line' may refer to a line of research or a lineage of drug development that traces back through various compounds and derivatives. It signifies the continuity of scientific inquiry that leads to the discovery and refinement of drug candidates within pharmacological studies.
7) Rheumatoid arthritis:
'Rheumatoid arthritis' is a chronic inflammatory disorder affecting joints. Research into pharmacological interventions for rheumatoid arthritis aims to relieve symptoms and halt disease progression. The significance of this condition underscores the need for novel anti-inflammatory agents that can provide substantial therapeutic benefits for patients.
8) Andhra (Amdhra):
'Andhra' refers to the Andhra Pradesh state in India. The mention of this region places the research within a specific geographical context, potentially highlighting local pharmaceutical research institutions or the contributions of researchers from this area to the global field of drug discovery.
9) India:
'India' is the country where the research and synthesis of isoxazolines are being conducted. The mention underscores India's active role in the pharmaceutical sciences and its contributions to global health through innovative drug development aimed at treating various diseases, including those prevalent in its population.
10) Species:
'Species' often refers to a specific group of organisms or bacteria. In pharmacology, understanding the diverse species of bacteria or pathogens is crucial for developing targeted treatments. Identifying how compounds interact with various species aids in developing broad-spectrum or targeted therapeutic agents.
11) Kanaka:
'Kanaka' is likely a reference to the author A. Kanaka Raju, indicating his contributions to the research within the article. It signifies the individual behind the study, reflecting the collaborative nature of scientific research and the importance of attribution in academic and clinical trials.
12) Barot:
'Barot' refers to a researcher involved in the synthesis of isoxazolines with reported antimicrobial activity. The mention emphasizes the contributions of individual scientists to the field of drug development, highlighting the collaborative nature of research and the significance of diverse inputs in advancing scientific knowledge.
13) Snake poison (Snake venom):
'Snake venom' refers to a complex mixture of toxic proteins secreted by snakes. The study of isoxazolines as potential inhibitors of snake venom enzymes demonstrates an innovative approach to pharmacology, seeking to develop therapeutic agents that can counteract the effects of venom in envenomated patients.
14) Pharmacological:
'Pharmacological' pertains to the science of drugs, including their actions, effects, and therapeutic potential. Understanding pharmacological aspects is critical in drug discovery, as it encompasses evaluating how drugs interact within biological systems, aiding in the development of effective and safe therapeutics for various diseases.
15) Tuberculosis:
'Tuberculosis' is a contagious bacterial infection primarily affecting the lungs. The significance of targeting tuberculosis in research underscores the need for effective treatments as drug-resistant strains emerge, necessitating ongoing studies into novel compounds, including isoxazolines, that may demonstrate efficacy against this serious health issue.
16) Inflammation:
'Inflammation' is a biological response to harmful stimuli, often resulting in redness, swelling, pain, and heat. The relevance of inflammation in pharmacology is vital, as many diseases involve inflammatory processes. Thus, developing compounds that can effectively manage inflammation represents a significant therapeutic goal in drug development.
17) Alleviation:
'Alleviation' refers to the act of making something less severe or more bearable, often in the context of symptoms related to disease. In pharmacology, the goal is to develop medications that can provide significant alleviation of symptoms for patients suffering from various ailments, improving their quality of life.
18) Transformation (Transform, Transforming):
'Transformed' typically refers to changes made to substances, often in a biological context where cells undergo alteration. In drug development, understanding how compounds transform within biological systems can inform their efficacy, safety, and potential side effects, making it a key concept in pharmacological research.
19) Srivastava (Sri-vastava, Shrivastava, Shri-vastava):
'Srivastava' likely refers to another contributing researcher in the synthesis of isoxazolines, emphasizing the collaborative effort involved in scientific inquiry. Acknowledging researchers like Srivastava reflects the importance of team contributions to advancements in pharmaceutical sciences and ensures appropriate attribution of scientific findings.
20) Shrinivasa (Shri-nivasa, Srinivasa):
'Srinivasa' is mentioned as a contributor to the research, possibly indicating co-authorship or collaboration. Reputable individuals in research highlight the collective expertise that drives advancements in drug discovery and development, influencing the course of scientific investigation and potential therapeutic outcomes.
21) Medicine:
'Medicine' refers to the science and practice of diagnosing, treating, and preventing disease. The exploration and synthesis of new compounds in pharmacology ultimately aim to produce advanced medicines that improve health outcomes, which underscores the importance of ongoing research in developing effective therapeutic agents.
22) Swelling:
'Swelling' is a common symptom of inflammation and injury, often addressed by anti-inflammatory drugs. In the context of pharmacological research, studying compounds that can effectively reduce swelling is crucial for developing treatments for various inflammatory conditions, enhancing therapeutic efficacy for patients.
23) Account:
'Account' in a research context refers to a summary or report of findings, methodologies, or observations. It signifies the importance of documenting research outcomes, allowing the scientific community to benefit from shared knowledge and advancements in drug development, fostering collaboration and further inquiry.
24) Cancer:
'Cancer' represents a group of diseases characterized by uncontrolled cell growth. Research into cancer treatments is critically important as the burden of cancer continues to grow globally. Drug discovery efforts, such as investigating isoxazolines, focus on developing compounds that can inhibit cancer cell proliferation, thereby enhancing treatment options.
25) Vasi (Vasin, Vashin, Vashi):
'Vashi' refers to a researcher mentioned in connection with the study of isoxazolines. This highlights individual contributions to scientific research and underscores the collaborative effort in pharmacological studies aimed at discovering new therapeutic agents with potential applications in treating various health conditions.
26) Ulcer:
'Ulcer' refers to a sore that develops on the lining of the stomach or intestines, often causing significant discomfort. The relevance of researching ulcer treatments reinforces the ongoing need for effective medications that alleviate symptoms and promote healing, emphasizing the role of pharmacological studies in addressing such conditions.
27) Field:
'Field' refers to a particular area of study or research, in this case, pharmaceutical sciences. Understanding the field's advancements, methodologies, and collaborative efforts is crucial for developing innovative treatments and enhancing healthcare practices, demonstrating the interconnectedness of various scientific disciplines in drug discovery.
28) Blood:
'Blood' plays a critical role in pharmacology, as it is the medium through which drugs are distributed throughout the body. Studying how drugs interact with blood and its components informs therapeutic strategies, especially for conditions related to the circulatory system and systemic diseases.
29) Study (Studying):
'Study' refers to the systematic investigation of compounds, diseases, or treatment methods. The importance of rigorous research studies in pharmacology cannot be overstated, as they provide empirical evidence needed to develop safe and effective drugs for various medical conditions, ultimately informing clinical practices.
30) Coral:
'Coral' in this context might refer to the research of compounds derived from marine sources. Coral-derived compounds may exhibit unique properties important in drug discovery, emphasizing the need for exploration and understanding of diverse natural products in developing novel therapeutic agents.
31) Fish:
'Fish' may allude to biological research involving aquatic organisms, often utilized as models for studying various diseases or environmental effects. The relevance of fish in pharmacological studies includes the investigation of drug efficacy and toxicity, contributing valuable insights into therapeutic strategies for both aquatic and human health.
32) Salt (Salty):
'Salt' refers to ionic compounds that can have various roles in pharmacology, such as stabilizing drug formulations or influencing the solubility and bioavailability of medications. Understanding the properties of salts used in drug preparation is important for optimizing pharmacological efficacy.
33) Viru:
'Viru' may refer to viruses or viral research, potentially in the context of developing antiviral medications. The study of viral infections and the exploration of compounds with antiviral properties are critical for enhancing therapeutic options against diseases caused by pathogenic viruses.