Synthesis of 3-hydroxy benzopyran thiazolidinones with antihypertensive effects.
Journal name: World Journal of Pharmaceutical Research
Original article title: Synthesis and characterization of various 3-(6- substituted-3-hydroxy-2,2-dimethyl-3,4-dihydro-2hbenzopyran- 4-yl)-2-substituted-1,3-thiazolidin-4-ones and their antihypertensive activity
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.
This page presents a generated summary with additional references; See source (below) for actual content.
Original source:
This page is merely a summary which is automatically generated hence you should visit the source to read the original article which includes the author, publication date, notes and references.
Soma Pramanik and Amit Kumar Das
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synthesis and characterization of various 3-(6- substituted-3-hydroxy-2,2-dimethyl-3,4-dihydro-2hbenzopyran- 4-yl)-2-substituted-1,3-thiazolidin-4-ones and their antihypertensive activity
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Copyright (license): WJPR: All rights reserved
Download the PDF file of the original publication
Summary of article contents:
1) Introduction
Hypertension, the most prevalent cardiovascular condition, significantly increases the risk of serious health issues such as coronary artery disease, heart failure, and stroke. The management of hypertension often requires a personalized approach to drug therapy, which must be adjusted based on various risk factors, including the severity of blood pressure elevation and the patient’s response to treatment. Traditional antihypertensive medications can result in adverse effects, necessitating the exploration of new therapeutic strategies. This study focuses on synthesizing and characterizing a series of novel benzopyran derivatives, known for their potential antihypertensive properties.
2) Synthesis of Benzopyran Derivatives
The research presented involved the development of 3-(6-substituted-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzopyran-4-yl)-2-substituted-1,3-thiazolidin-4-ones using a methodical synthetic approach that included acylation, Fries rearrangement, cyclization, reduction, epoxidation, and Schiff’s reaction. The synthesis began with the acylation of substituted phenols to produce acetophenones, which were subsequently converted to benzopyran derivatives. The compounds were characterized using advanced spectroscopic techniques including IR, NMR, and mass spectrometry, confirming their structure and purity.
3) Antihypertensive Mechanisms of Benzopyran
Benzopyran analogues act as potassium channel openers, facilitating the relaxation of vascular smooth muscle and potentially leading to lower blood pressure. The study highlighted that compounds like cromakalim have demonstrated efficacy in achieving myorelaxation by activating ATP-sensitive potassium (KATP) channels. Benzopyrans exhibit a similar effect, indicating their capability to serve as effective antihypertensive agents. This mechanism is significant because it offers a potentially novel pathway through which hypertension can be effectively managed, especially in patients intolerant to traditional therapies.
4) In Vivo Antihypertensive Activity Testing
The synthesized benzopyran derivatives were subjected to in vivo pharmacological screening using male Albino Wistar rats induced with fructose-based hypertension. The compounds were administered, and subsequent measurements of blood pressure were evaluated employing a non-invasive tail cuff method. Results indicated that the synthesized molecules successfully mitigated the increases in blood pressure caused by high fructose intake. The study demonstrated marked reductions in systolic and diastolic blood pressures, proving the antihypertensive efficacy of the novel compounds.
5) Conclusion
The high prevalence of hypertension and its severe implications on global health underscore the necessity for innovative therapeutic options. This study successfully synthesized a series of benzopyran derivatives with proven antihypertensive activity via mechanisms that regulate potassium channels. The results emphasize the need for further investigation into this class of compounds to develop more effective, less toxic antihypertensive agents. Continued research in this area could play a pivotal role in combating the escalating global hypertension crisis, ultimately improving cardiovascular health outcomes.
FAQ section (important questions/answers):
What was the objective of the study by Soma et al.?
The study aimed to synthesize and characterize novel 3-(6-substituted-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzopyran-4-yl)-2-substituted-1,3-thiazolidin-4-ones and evaluate their antihypertensive activity in fructose-induced hypertensive rats.
Which methods were used for compound synthesis in the study?
The synthesis involved various methods including acylation, Fries rearrangement, cyclisation, reduction, and Schiff’s reaction, utilizing substituted phenols as starting materials.
How was the antihypertensive activity tested in the study?
Antihypertensive activity was tested in fructose-induced hypertensive rats using the tail-cuff method to measure blood pressure before and after administering the synthesized compounds.
What findings were reported regarding the antihypertensive effects of the compounds?
The study found that synthesized compounds significantly reduced blood pressure in fructose-induced hypertensive rats, leading to levels comparable to control values.
What modern techniques validated the structures of synthesized compounds?
The structures were validated using various spectroscopic techniques including 1H NMR, mass spectrometry, and FT-IR spectroscopy.
Why is hypertension considered a significant health risk?
Hypertension is a major risk factor for serious conditions such as coronary artery disease, heart failure, stroke, and renal failure, contributing to global cardiovascular disease prevalence.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Synthesis of 3-hydroxy benzopyran thiazolidinones with antihypertensive effects.”. 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) Channel:
In pharmacology, specifically regarding the antihypertensive activity being explored, the term 'channel' refers to protein structures in cell membranes that facilitate the movement of ions, such as potassium (K+). Potassium channels play a crucial role in regulating cardiovascular functions and can influence blood pressure levels when modulated by drugs, making the study of channel openers vital for developing antihypertensive therapies.
2) Water:
Water is commonly used in biomedical research for various purposes, including diluting substances, preparing solutions, and serving as a solvent in chemical reactions. In the context of the study, water is significant as the medium for administering fructose to rats, which induces hypertension and serves as part of the experimental setup to assess antihypertensive efficacy.
3) Soma:
Soma Pramanik is a key author of the research study that investigates benzopyran derivatives and their antihypertensive activity. The research contributions made by Pramanik and co-researchers involve synthesizing new compounds and evaluating their effects on blood pressure, reflecting their role in advancing pharmacological knowledge and therapies against hypertension.
4) Activity:
Activity in this context refers to the biological efficacy of synthesized benzopyran derivatives in lowering blood pressure. The study explored the 'in vivo' antihypertensive activity in rat models, highlighting the importance of assessing how chemical compounds interact with physiological processes to validate their therapeutic potential.
5) Blood:
Blood is a vital fluid that circulates in the body, carrying nutrients and oxygen to tissues while removing waste products. In the context of the study, measuring blood pressure (both systolic and diastolic) is essential to determine the effectiveness of the synthesized compounds, establishing a direct correlation between drug administration and cardiovascular health.
6) Drug:
In this research, 'drug' refers to the synthesized chemical compounds derived from benzopyrans, aimed at exhibiting antihypertensive properties. The study grapples with the efficacy, side effects, and potential benefits of these drugs in treating hypertension, contributing to the ongoing search for newer, safer antihypertensive agents.
7) Disease:
Disease, particularly hypertension, is the primary focus of the study. Hypertension is a significant health condition linked to various cardiovascular issues and, thus, the research aims to identify new therapeutic agents that can effectively manage and mitigate the adverse effects associated with this prevalent disease.
8) Animal:
Animal models, specifically male Albino Wistar rats in this study, are essential for preclinical testing of new drugs. Using animals enables researchers to observe the biological effects of synthesized compounds in a controlled environment, providing insights into their potential efficacy and safety before human trials.
9) Table:
Table refers to the organized presentation of data that summarizes research findings. In this study, tables display various results, including spectral data, antihypertensive activity, and other analytical outcomes. Tables facilitate easier comparison of results and provide a clear overview of the effects of different compounds on blood pressure.
10) Pharmacological:
Pharmacological pertains to the branch of medicine that studies drug action and how drugs affect biological systems. The research involves understanding the pharmacological effects of new benzopyran derivatives, focusing on their mechanism of action, dosage effectiveness, and side effects, contributing to the development of antihypertensive agents.
11) Karnataka:
Karnataka is the Indian state where the research takes place. The location serves as a significant backdrop for the study, providing resources such as skilled researchers, laboratory facilities, and institutional support that enable scientific investigations in the field of pharmaceutical chemistry and public health in India.
12) India:
India serves as the context for the research, both geographically and culturally, reflecting local healthcare challenges such as the high prevalence of hypertension. The findings could inform better local health policies and treatment strategies while contributing to the global understanding of hypertension management.
13) Death:
Death is a critical outcome linked to untreated hypertension, as it can lead to fatal cardiovascular diseases, stroke, and renal failure. By understanding and addressing hypertension through pharmacological research, the study aims to contribute to reducing morbidity and mortality associated with this condition.
14) Study (Studying):
The study represents a systematic investigation into the synthesis and evaluation of novel antihypertensive compounds. It encompasses methodologies, results, and implications of the research findings, aiming to advance the pharmaceutical field and contribute to better hypertension management strategies.
15) Diet:
Diet refers to the nutritional intake and regimens that can influence health and Hypertension. The study assesses the impact of a high-fructose diet in inducing hypertension in rat models, reflecting the importance of nutrition in cardiovascular health and the role of lifestyle changes in managing disease.
16) Road:
Road, in this context, may refer to the colloquial path or journey in scientific research, indicating the process of discovery, experimentation, and development in creating new antihypertensive therapies. It symbolizes the progression from conceptual ideas to practical applications in medicine.
17) Measurement:
Measurement pertains to the quantification of blood pressure and other physiological parameters during the study. Accurate and consistent measurements are essential for evaluating the efficacy of antihypertensive agents and ensuring the reliability of research findings.
18) Discussion:
Discussion reflects the interpretation and analysis of the research findings. In the context of this study, it provides insights on the implications of the results, suggesting how findings relate to existing literature and their potential impact on future antihypertensive drug development.
19) Science (Scientific):
Scientific refers to the rigorous methods and principles applied in the research. The study employs established scientific techniques for synthesizing compounds and evaluating their effects, adhering to methodological standards that ensure the credibility and reproducibility of the findings.
20) Toxicity:
Toxicity is a critical factor considered when developing new drugs. The study addresses potential adverse effects of synthesized compounds, examining their safety profiles to ensure that new antihypertensive agents do not produce harmful consequences, allowing safer therapeutic options for patients.
21) Surface:
Surface might indicate the physical characteristics of substances, particularly in the context of compound formulation or during measurement procedures. Clean surfaces, for instance, are pertinent to ensure the reliability of blood pressure measurements and avoid erroneous results.
22) Purity:
Purity refers to the quality of synthesized compounds being free from contaminants or by-products. It is a crucial aspect in pharmaceutical research, as impurities can affect drug efficacy, safety, and overall research outcomes; thus, purity assessments are routinely incorporated into experimental protocols.
23) Powder:
Powder symbolizes the physical form that synthesized compounds might take during the research. Many pharmaceutical substances are formulated as powders to facilitate dosing, aiding in solid-state characterization and enabling various analytical techniques to evaluate their properties effectively.
24) Cotton:
Cotton is commonly used for laboratory procedures, such as cleaning the surfaces for blood pressure measurement. In research, it also acts as a practical tool for managing contamination and ensuring accuracy in performing various scientific techniques.
25) Kumar:
Amit Kumar Das is a co-author of the research study, indicating his involvement in the investigation of antihypertensive activity of synthesized benzopyran derivatives. Collaborative efforts among researchers like Das contribute to expanding knowledge and improving outcomes in pharmaceutical sciences.
26) Pulse:
Pulse in the context of this study likely references the methodology used to monitor blood pressure in rat models through the tail-cuff method. Accurate pulse measurements are vital for understanding cardiovascular health and assessing the effectiveness of antihypertensive compounds.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Synthesis of 3-hydroxy benzopyran thiazolidinones with antihypertensive effects.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Alcohol consumption, Pharmacological activity, Cardiovascular disease, Weight reduction, Global Burden, TLC, Mass spectrometry, Analytical data, Column chromatography, Anti-hypertensive activity, Mean arterial blood pressure, Ethyl Acetate, Pharmacological profile, Antihypertensive Activity, Albino Wistar rats, Sodium Carboxy Methyl Cellulose, Analytical technique, Potassium intake, Treatment of hypertension, High Prevalence, Toxic compound, Synthetic compound.