Structural modifications enhance analgesic activity and ADME of 4-hydroxy 4-phenyl piperidine.
Journal name: World Journal of Pharmaceutical Research
Original article title: The structural modification causes the enhancement of analgesic activity of 4-hydroxy 4- phenyl piperidine along with an excellent interaction with digestive enzyme, leading good adme
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Kiran Rafiq, Zafar Saied Saify, Asghari Ghous, Shazia Haider , Nighat Sultana
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: The structural modification causes the enhancement of analgesic activity of 4-hydroxy 4- phenyl piperidine along with an excellent interaction with digestive enzyme, leading good adme
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study conducted by Kiran et al. explores the enhancement of analgesic activity in 4-Hydroxy-4-Phenyl Piperidine derivatives, alongside their interaction with the digestive enzyme amylase. Piperidine compounds have gained notoriety in the pharmacological field for their therapeutic significance, particularly in analgesia. Synthetic derivatives, inspired by the structural properties of well-known opioid analgesics like pethidine and fentanyl, were assessed for their pain-relieving effects through various experimental methods, ultimately showcasing modifications to their core structure that contributed to improved pharmacological properties.
Enhancement of Analgesic Activity
The research highlights the effectiveness of synthesized derivatives of 4-Hydroxy-4-Phenyl Piperidine as potent analgesics. Using animal models, specifically albino mice, the analgesic activity was measured using Eddy’s hot plate method at a dosage of 50 mg/kg. The study found that various derivatives exhibited significantly enhanced analgesic responses compared to the parent compound. The substitution of a methyl group at the nitrogen atom in the piperidine ring was identified as a critical factor in amplifying the analgesic potency. Notably, the derivatives displayed strong analgesic effects consistently throughout the assessment period, indicating their potential application in pain management.
Interaction with Digestive Enzyme Amylase
An additional aspect of the research focused on the compatibility of these synthesized piperidine derivatives with the digestive enzyme alpha-amylase. The in vitro antiamylatic activity was assessed using an agar plate method, which allowed the researchers to determine the inhibition area caused by the compounds. The results indicated that not only did the synthesized derivatives show moderate inhibitory effects, but they also appeared to enhance amylase activity, promoting potential benefits for oral administration and bioavailability. Consequently, this relationship reinforces the importance of structural modifications to improve both analgesic effectiveness and enzymatic compatibility, aiding in drug absorption.
Structure-Activity Relationship (SAR) Insights
The study also delves into the structural activity relationship (SAR) of the synthesized compounds. By examining how variations in molecular structure influence analgesic activity, the authors concluded that certain modifications, specifically the introduction of a methyl group, significantly impacted the analgesic response without affecting the duration of the analgesic effect. This deeper understanding of the binding interactions between the opioid receptors and the modified compounds may pave the way for more effective analgesic agents with fewer side effects. The research emphasizes the critical role of molecular structure in designing new therapeutic agents.
Conclusion
In conclusion, Kiran et al.’s research presents compelling evidence for the potential of modified piperidine derivatives as effective analgesic agents and their favorable interactions with digestive enzymes. With enhanced analgesic properties attributable to specific structural modifications, these compounds demonstrate promising avenues for further development in pain relief therapies. The findings not only contribute valuable insights into the pharmacological potential of piperidine derivatives but also underscore the criticality of structural optimization in drug development. Continued exploration of these derivatives could yield new, effective pain management solutions with improved bioavailability and efficacy.
FAQ section (important questions/answers):
What was the purpose of the study on piperidine derivatives?
The study aimed to evaluate the analgesic activity of synthesized derivatives of 4-Hydroxy-4-Phenyl Piperidine compared to the standard drug Pethidine in a mouse model.
How was analgesic activity measured in the experiment?
Analgesic activity was measured using the hot plate method, assessing the latency of pain response in treated mice at various time intervals after administration.
What was the effect of structural modifications on analgesic efficacy?
Structural modifications of the parent compound resulted in enhanced analgesic potency, with various derivatives demonstrating significant analgesic effects in comparison to the parent molecule.
What method was used to evaluate the interaction with amylase?
The interaction of synthesized compounds with alpha-amylase was assessed using an agar plate method, measuring inhibition zones to determine compatibility with the enzyme.
Which compounds exhibited the best analgesic response?
Compounds such as 1-(1′�-Phenoxypropyl)-4-phenyl-4-hydroxy piperidinium Hydrobromide and others showed significant analgesic responses after 30 minutes and sustained effects thereafter.
What were the results regarding interaction with alpha-amylase?
All synthesized derivatives showed significant interaction with alpha-amylase, enhancing enzymatic activity and indicating good compatibility without disrupting the enzyme's pharmacological behavior.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Structural modifications enhance analgesic activity and ADME of 4-hydroxy 4-phenyl piperidine.�. 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 pharmacology, 'activity' pertains to the effectiveness of a drug or compound in eliciting a specific biological response. In this study, the analgesic activity of synthesized derivatives is evaluated through experimental methods, indicating their potential to alleviate pain in various tested models.
2) Drug:
'Drug' refers to any substance used for therapeutic purposes to diagnose, cure, treat, or prevent diseases. In this research, synthetic derivatives of the piperidine compound are emphasized for their analgesic properties, highlighting their role in pain management and therapeutic applications.
3) Table:
'Table' refers to a structured representation of data for easy comparison and analysis. In the study, tables summarize the experimental results regarding analgesic effects and antiamylatic activity of different compounds, providing clear insights into their efficacy and interaction with target enzymes.
4) Study (Studying):
'Studying' refers to the act of learning or investigating a particular topic in-depth. In the scope of this paper, studying involves experimental methods to explore the analgesic properties of synthesized piperidine compounds and their interactions with enzymes, contributing to knowledge in pharmaceutical sciences.
5) Pharmacological:
'Pharmacological' relates to the branch of medicine that deals with the interactions between drugs and biological systems. The term is significant in the article because it pertains to the understanding of how synthesized compounds affect biological functions, particularly regarding pain relief and enzyme interaction.
6) Animal:
'Animal' refers to living organisms used in research to understand biological processes and test drugs' safety and efficacy. In this study, mice are utilized as subjects for assessing the analgesic effects of the synthesized piperidine derivatives, which reflect the compounds' potential therapeutic efficacy.
7) Pain (Pai�):
'Pain' is an unpleasant sensory and emotional experience associated with actual or potential tissue damage. The study emphasizes the role of piperidine derivatives as analgesics, aiming to provide therapeutic relief for pain by working on specific receptors in the nervous system.
8) Similarity:
'Similarity' indicates the degree to which two or more entities resemble each other in structure or function. In this context, the similarity between piperidine derivatives and known opioids like morphine is highlighted, suggesting potential for therapeutic effectiveness in pain alleviation based on structural characteristics.
9) Water:
'Water' is a vital solvent in biological systems and serves as a medium for various physiological processes. In pharmacological studies, the role of water is often related to the preparation of solutions for testing compounds, indicating its importance in drug formulation and interaction assessments.
10) Inflammation:
'Inflammation' is a biological response to harmful stimuli, often causing pain, swelling, and redness. The study explores analgesic compounds targeting pain relief, making inflammation a relevant factor, as many analgesics are prescribed to alleviate pain associated with inflammatory conditions.
11) Discussion:
'Discussion' involves analyzing and interpreting the results of a study. In this research, the discussion section would likely encapsulate the effectiveness of synthesized derivatives in pain management and their pharmacological interactions, contextualizing findings within existing literature and proposing future research directions.
12) Company:
'Company' often refers to a business entity involved in developing or marketing drugs. In this article, 'company' relates to the sourcing of compounds or materials necessary for experimentation, highlighting the collaborative aspect of pharmaceutical research and development in the context of drug discovery.
13) Dealing:
'Dealing' refers to the process of managing or handling interactions within a particular context. In pharmacology, it can relate to the interactions between drugs and biological systems, addressing how synthesized compounds effectively manage or mitigate pain and interact with digestive enzymes.
14) Nature:
'Nature' signifies the intrinsic qualities or characteristics of substances or systems. In the study, it may refer to the chemical nature of the synthesized piperidine derivatives and their biological behavior, affecting how they function as analgesics and interact with enzymes within physiological contexts.
15) Glass:
'Glass' commonly indicates the material used for laboratory equipment, such as petri dishes or test tubes. In this study, glass apparatus would contextually represent tools required during experimentation for handling compounds, thereby facilitating analysis of their pharmacological and biological properties.
16) Ulcer:
'Ulcer' refers to a sore that develops on the lining of the stomach or the intestine. In this research context, the effects of piperine from black pepper on ulcers are noted, emphasizing the gastoprotective properties of certain compounds and their relevance in digestive health.
17) Bile:
'Bile' is a digestive fluid produced by the liver to help in breaking down fats. In the study, its mention indicates investigations into how piperidine derivatives may influence digestive processes, specifically their potential role in enhancing bile secretion for better fat metabolism.
18) Diet:
'Diet' encompasses the types and quantities of food consumed. In pharmacological studies, diet can affect drug absorption and metabolism, thus influencing the efficacy of the synthesized analgesic compounds when administered in conjunction with dietary considerations during research.
Other Science Concepts:
Discover the significance of concepts within the article: �Structural modifications enhance analgesic activity and ADME of 4-hydroxy 4-phenyl piperidine.�. Further sources in the context of Science might help you critically compare this page with similair documents:
Statistical analysis, Bioavailability, Analgesic effect, Animal model, Analgesic activity, Zone of inhibition, Piperine, Antinociceptive activity, Effective dose, Eddy's hot plate method, Potent analgesic, Structure-activity relationship, Opioid Analgesic, Hot plate method, Therapeutically Active Molecules, Agar plate method, Wistar rat, Digestive Enzyme, Pethidine, Antinociceptive effect, Salivary secretion, Pharmacological behavior.