Exploring the Chemistry and Therapeutic Potential of Triazoles: A Comprehensive Literature Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1298-1368 ◽  
Author(s):  
Ankit Jain ◽  
Poonam Piplani
Keyword(s):  
Oxidative Stress ◽  
Drug Discovery ◽  
Literature Review ◽  
Structural Modification ◽  
Therapeutic Potential ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Triazole Derivatives ◽  
Comprehensive Literature Review ◽  
The Common

: Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.

scholarly journals Resilience Assessment Frameworks of Critical Infrastructures: State-of-the-Art Review

Buildings ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 464
Author(s):  
Dan Guo ◽  
Ming Shan ◽  
Emmanuel Kingsford Owusu
Keyword(s):  
Literature Review ◽  
Natural Disasters ◽  
State Of The Art ◽  
Future Research ◽  
Critical Infrastructures ◽  
The Past ◽  
Comprehensive Literature Review ◽  
The Common ◽  
Key Indicators ◽  
Resilience Assessment

During the past two decades, critical infrastructures (CIs) faced a growing number of challenges worldwide due to natural disasters and other disruptive events. To respond to and handle these disasters and disruptive events, the concept of resilience was introduced to CIs. Particularly, many institutions and scholars developed various types of frameworks to assess and enhance CI resilience. The purpose of this paper is to review the resilience assessment frameworks of the CIs proposed by quality papers published in the past decade, determine and analyze the common dimensions and the key indicators of resilience assessment frameworks of CIs, and propose possible opportunities for future research. To achieve these goals, a comprehensive literature review was conducted, which identified 24 resilience assessment frameworks from 24 quality papers. This paper contributes to the current body of resilience research by identifying the common dimensions and the key indicators of the resilience assessment frameworks proposed for CIs. In addition, this paper is beneficial to the practice, because it provides a comprehensive view of the resilience assessment frameworks of CIs from the perspective of implementation, and the indicators are pragmatic and actionable in practice.

Chyavanprash: Choice of Drug for immunity boosting and health supplements during COVID -19 pandemic

2020 ◽  
Vol 11 (SPL1) ◽  
pp. 1346-1350
Author(s):  
Bharat Rathi ◽  
Renu Rathi ◽  
Vinod Ade ◽  
Akshay Pargaonkar
Keyword(s):  
Therapeutic Potential ◽  
Age Groups ◽  
Pharmacological Activities ◽  
Common People ◽  
The World ◽  
The Common ◽  
Made In ◽  
Health Supplements

Chyavanprash a known Ayurvedic formulation formulated by sage Chyavan to impart youth, charm, strength & prolonged life. It is very much valued for possessing numerous health benefits with respect to the preventive, curative and promotive aspects of health. Chyavanprash can be consumed throughout the year. Several scientific evidences support its wholesome and safe healthy tonic status that is favorable for all age groups and genders alike. In modern days, it has gained mammoth popularity throughout the world. CP is prepared with Amalaki (Emblica officinalis) as a prime drug with other nutrient rich herbs help to preserve stamina, strength and vitality. Various pre clinical (in vivo & in vitro), Experimental, Analytical and clinical studies conducted on CP and its individual components revealed its various pharmacological activities most of which are suggestive of immunity enhancer and health supplements. Hence an attempt is made in the present paper to find out and explore the scientific evidences based on therapeutic potential of CP with respect to immunity and health supplements and make evidences available to the common people to combat the COVID-19 menace effectively.

Evaluation of the pharmacological properties of piscine venoms from both Lionfish (Pterois) and Stonefish (Synanceja)

2020 ◽  
Vol 16 ◽  
Author(s):  
Karthikeyan Ramalingam
Keyword(s):  
Drug Discovery ◽  
Cell Membrane ◽  
Pharmaceutical Research ◽  
Cross Reactivity ◽  
Future Research ◽  
Neuromuscular System ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
The Past ◽  
Neuromuscular Systems

Background:: For the past 70 years, the focus of research is towards the search for poisons and toxins found in venomous and poisonous organisms which is purely directed towards the pharmacological properties of the toxins. In the research of finding novel compounds in pharmaceutical research, the identified source was the piscine venom. Objective:: Scorpanidae family was considered the most venomous of all. The toxins isolated from stonefish and lionfish are responsible for the effects caused in cardiovascular and neuromuscular systems and also in causing cytolytic activities. The main objective of the review is to study the mechanism of the stone fish venom and portray its benefits in the field of drug discovery. Methods:: A study on the mechanism of stone fish venom was carried out by inducing cardiovascular endothelium. The release of neurotransmitter signals thus leads to the depolarisation of cell membrane by the formation of pores in the cell membrane in neuromuscular system of rabbits, porcine artery, mice and rats. Lionfish venom in cross reactivity with the results evolved from a stonefish venom activity. The presence of enzymatic hyaluronidase in the primary structures of lionfish has evolved from stonefish and their anticancer potential has also been demonstrated for the benefits of drug discovery as they possess biological and chemical activity. Conclusion:: This review depicts an overview on the pharmacological activities of lionfish venom in comparison with the stonefish venom and their purpose on applications for future research in drug discovery.

scholarly journals Harnessing Pivotal Advances for Production and Structural Derivation of the Promising Molecule Ursolic Acid

2021 ◽  
Author(s):  
Hao-ran Liu ◽  
Nadeem Ahmad ◽  
Bo Lv ◽  
Chun Li
Keyword(s):  
Ursolic Acid ◽  
Large Scale ◽  
Structural Modification ◽  
Therapeutic Potential ◽  
Scale Production ◽  
Pharmacological Activities ◽  
Significant Safety ◽  
Pentacyclic Triterpenoid ◽  
Large Scale Production ◽  
Vast Range

Ursolic acid (UA) is a ursane-type pentacyclic triterpenoid compound, naturally produced in plants via specialized metabolism and exhibits vast range of remarkable physiological activities and pharmacological manifestations. Owing to significant safety and efficacy in different medical conditions, UA may serve as a backbone to produce its derivatives with novel therapeutic functions. This review systematically provides an overview of the pharmacological activities, acquisition methods and structural modification methods of UA. In addition, we focused on the synthetic modifications of UA to yield its valuable derivatives with enhanced therapeutic potential. Furthermore, harnessing the essential advances for green synthesis of UA and its derivatives by advent of metabolic engineering and synthetic biology are highlighted. In combination with the advantages of UA biosynthesis and transformation strategy, large-scale production and applications of UA is a promising platform for further exploration.

Coumarin-Oxadiazole Derivatives: Synthesis and Pharmacological Properties

2020 ◽  
Vol 17 (7) ◽  
pp. 780-794
Author(s):  
Nurhayatun S. Abdul Razak ◽  
Joazaizulfazli Jamalis ◽  
Subhash Chander ◽  
Roswanira Abdul Wahab ◽  
Deepak P. Bhagwat ◽  
...  
Keyword(s):  
Natural Products ◽  
Clinical Practice ◽  
Review Paper ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Oxadiazole Derivatives ◽  
The Common

Coumarin and oxadiazole moieties ubiquitously occur in a wide range of natural products and are valued for their varied and beneficial pharmacological activities. Herein, this review focuses on various documented techniques used by researchers to synthesize an assortment of biologically active coumarin-oxadiazole scaffolds. Also, the common techniques discussed are used to establish the wide-range of biological activities of the synthesized coumarin and oxadiozole derivatives, including; antioxidant, anthelmintic, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, cytotoxicity and anticonvulsant. Additionally, the current, well-established drugs synthesized using coumarin-oxadiazole scaffolds are typically dispensed in regular clinical practice are also highlighted in this review paper.

scholarly journals Therapeutic Potential of α- and β-Pinene: A Miracle Gift of Nature

Biomolecules ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 738 ◽  
Author(s):  
Bahare Salehi ◽  
Shashi Upadhyay ◽  
Ilkay Erdogan Orhan ◽  
Arun Kumar Jugran ◽  
Sumali L.D. Jayaweera ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antibiotic Resistance ◽  
Biological Activity ◽  
Therapeutic Potential ◽  
Clinical Applications ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Analgesic Effects ◽  
Wide Range ◽  
Resistance Modulation

α- and β-pinene are well-known representatives of the monoterpenes group, and are found in many plants’ essential oils. A wide range of pharmacological activities have been reported, including antibiotic resistance modulation, anticoagulant, antitumor, antimicrobial, antimalarial, antioxidant, anti-inflammatory, anti-Leishmania, and analgesic effects. This article aims to summarize the most prominent effects of α- and β-pinene, namely their cytogenetic, gastroprotective, anxiolytic, cytoprotective, anticonvulsant, and neuroprotective effects, as well as their effects against H2O2-stimulated oxidative stress, pancreatitis, stress-stimulated hyperthermia, and pulpal pain. Finally, we will also discuss the bioavailability, administration, as well as their biological activity and clinical applications.

scholarly journals Therapeutic Potential of Lindera obtusiloba: Focus on Antioxidative and Pharmacological Properties

Plants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1765
Author(s):  
Md Ezazul Haque ◽  
Shofiul Azam ◽  
Rengasamy Balakrishnan ◽  
Mahbuba Akther ◽  
In-Su Kim
Keyword(s):  
Oxidative Stress ◽  
Blood Circulation ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Pharmacological Properties ◽  
Asian Countries ◽  
Traditional Use ◽  
Active Constituents ◽  
Lead Compounds ◽  
Lindera Obtusiloba

Lindera obtusiloba (LO) BLUME from the genus Lindera (Lauraceae) is a medicinal herb traditionally used in Southeast Asian countries. Indigenously, extracts of different parts of the plant have been used to improve blood circulation and treat allergy, inflammation, rheumatism, and liver diseases. LO is a rich source of therapeutically beneficial antioxidative phytochemicals, such as flavonoids, butenolides, lignans and neolignans. Moreover, recent studies have unravelled the pharmacological properties of several newly found active constituents of LO, such as anti-inflammatory antioxidants (+)-syringaresinol, linderin A, anti-atherosclerotic antioxidant (+)-episesamin, anti-melanogenic antioxidants quercitrin and afzelin, cytotoxic 2-(1-methoxy-11-dodecenyl)-penta-2,4-dien-4-olide, (2Z,3S,4S)-2-(11-dodecenylidene)-3-hydroxy-4-methyl butanolide, anti-allergic koaburaside, (6-hydroxyphenyl)-1-O-beta-d-glucopyranoside and 2,6-dimethoxy-4-hydroxyphenyl-1-O-beta-d-glucopyranoside and the antiplatelet-activity compound Secolincomolide A. These findings demonstrate that LO can be a potential source of antioxidants and other prospective therapeutically active constituents that can lead to the development of oxidative stress-mediated diseases, such as cardiovascular disorders, neurodegenerative disorders, allergies, inflammation, hepatotoxicity, and cancer. Here, the antioxidant properties of different species of Lindera genus are discussed briefly. The traditional use, phytochemistry, antioxidative and pharmacological properties of LO are also considered to help researchers screen potential lead compounds and design and develop future therapeutic agents to treat oxidative stress-mediated disorders.

scholarly journals Recent Updates on the Synthesis of Bioactive Quinoxaline-Containing Sulfonamides

2021 ◽  
Vol 11 (12) ◽  
pp. 5702
Author(s):  
Ali Irfan ◽  
Sajjad Ahmad ◽  
Saddam Hussain ◽  
Fozia Batool ◽  
Haseeba Riaz ◽  
...  
Keyword(s):  
Literature Review ◽  
Biomedical Applications ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Activities ◽  
Lead Compounds ◽  
Structure Activity ◽  
Wide Range ◽  
Sulfonamide Group

Quinoxaline is a privileged pharmacophore that has broad-spectrum applications in the fields of medicine, pharmacology and pharmaceutics. Similarly, the sulfonamide moiety is of considerable interest in medicinal chemistry, as it exhibits a wide range of pharmacological activities. Therefore, the therapeutic potential and biomedical applications of quinoxalines have been enhanced by incorporation of the sulfonamide group into their chemical framework. The present review surveyed the literature on the preparation, biological activities and structure-activity relationship (SAR) of quinoxaline sulfonamide derivatives due to their broad range of biomedical activities, such as diuretic, antibacterial, antifungal, neuropharmacological, antileishmanial, anti-inflammatory, anti-tumor and anticancer action. The current biological diagnostic findings in this literature review suggest that quinoxaline-linked sulfonamide hybrids are capable of being established as lead compounds; modifications on quinoxaline sulfonamide derivatives may give rise to advanced therapeutic agents against a wide variety of diseases.

Pneumomediastinum: A Rare Presentation of Inflicted Injuries in Infants

2020 ◽  
Author(s):  
Adam Lee ◽  
Adam Bajinting ◽  
Abby Lunneen ◽  
Colleen M. Fitzpatrick ◽  
Gustavo A. Villalona
Keyword(s):  
Literature Review ◽  
Retrospective Review ◽  
Review Of The Literature ◽  
Rare Presentation ◽  
Spontaneous Pneumomediastinum ◽  
Nonaccidental Trauma ◽  
Comprehensive Literature Review ◽  
Healthy Infants ◽  
History Of

AbstractReports of incidental pneumomediastinum in infants secondary to inflicted trauma are limited. A retrospective review of infants with pneumomediastinum and history of inflicted trauma was performed. A comprehensive literature review was performed. Three infants presented with pneumomediastinum associated with inflicted trauma. Mean age was 4.6 weeks. All patients underwent diagnostic studies, as well as a standardized evaluation for nonaccidental trauma. All patients with pneumomediastinum were resolved at follow-up. Review of the literature identified other cases with similar presentations with related oropharyngeal injuries. Spontaneous pneumomediastinum in previously healthy infants may be associated with inflicted injuries. Clinicians should be aware of the possibility of an oropharyngeal perforation related to this presentation.

Phosphino-Triazole Ligands for Palladium-Catalysed Cross-Coupling

2018 ◽  
Author(s):  
Yiming Zhao ◽  
Huy van Nguyen ◽  
Louise Male ◽  
Philip Craven ◽  
Benjamin R. Buckley ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cross Coupling ◽  
Product Formation ◽  
Coupling Reactions ◽  
Volume Determination ◽  
Online Tool ◽  
Triazole Derivatives ◽  
Cross Coupling Reactions ◽  
Modelling Approaches

<div>Twelve 1,5-disubtituted and fourteen 5-substituted 1,2,3-triazole derivatives bearing diaryl or dialkyl phosphines at the 5-position were synthesised and used as ligands for palladium-catalysed Suzuki-Miyaura cross-coupling reactions. Bulky substrates were tested, and lead-like product formation was demonstrated. The online tool SambVca 2.0 was used to assess steric parameters of ligands and preliminary buried volume determination using XRD obtained data in a small number of cases proved to be informative. Two modelling approaches were compared for the determination of</div><div>the buried volume of ligands where XRD data was not available. An approach with imposed steric restrictions was found to be superior in leading to buried volume determinations that closely correlate with observed reaction conversions. The online tool LLAMA was used to determine lead-likeness of potential Suzuki-Miyaura cross-coupling products, from which ten of the most lead-like were successfully synthesised. Thus, confirming these readily accessible triazole-containing phosphines as highly suitable ligands for reaction screening and optimisation in drug discovery campaigns.</div>

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