A comprehensive overview of the medicinal chemistry of antifungal drugs: perspectives and promise

2020 ◽  
Vol 49 (8) ◽  
pp. 2426-2480 ◽  
Author(s):  
Kaitlind C. Howard ◽  
Emily K. Dennis ◽  
David S. Watt ◽  
Sylvie Garneau-Tsodikova
Keyword(s):  
Fungal Pathogens ◽  
Medicinal Chemistry ◽  
Antifungal Drugs ◽  
Comprehensive Overview ◽  
The World

The emergence of new fungal pathogens makes the development of new antifungal drugs a medical imperative that in recent years motivates the talents of numerous investigators across the world.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

In vitro evaluation of the anti-mycobacterial properties of the extracts of Momordica Charantia

2021 ◽  
Vol 16 (7) ◽  
pp. 15-22
Author(s):  
Paul Giftson ◽  
Jerrine Joseph ◽  
Revathy Kalyanasundaram ◽  
V. Ramesh Kumar ◽  
Wilson Aruni
Keyword(s):  
Medicinal Plants ◽  
Fungal Pathogens ◽  
Communicable Disease ◽  
Antimycobacterial Activity ◽  
Bitter Gourd ◽  
World Population ◽  
Methanol Extracts ◽  
Crude Extracts ◽  
The World

Tuberculosis (TB) is a communicable disease and remains one of the top 10 causes of death worldwide. One fourth of the world population is infected with TB at a risk of developing disease. The increase in the incidence of drug resistant TB around the world urges the need to develop a new candidate to fight against the disease. Plants were considered as the rich source of bioactive components to be used as potential drugs. Medicinal plants are used in pure as well as crude materials for their medicinal properties. Our research aims in identifying the phyto-molecules which have anti- tuberculosis property. Four medicinal plants namely, Acalyphaciliata (Kuppaimeni), Solanumtrilobatum (Thuthuvalai), Momordicacharantia (Bitter Gourd) and Sennaauriculata (Avaram) were chosen to evaluate their antimicrobial activity focusing on anti-tubercular activity. The methanol extracts of the medicinal plants showed significant inhibitory activity against bacterial and fungal pathogens. Sennaauriculata methanol extracts showed activity against S. aureus, E. coli, P. aeruginosa and C. albicans. In the screening of antimycobacterial activity done by LRP assay, among the plant extracts tested, the hexane crude extracts of Momordicacharantia (Bitter Gourd) showed 82.2% and 81.03% of inhibition against M. tuberculosis H37Rv at 500µg/ml and 250µg/ml concentration respectively. Similarly, the methanol crude extracts of Momordicacharantia showed 87.14% and 63.55% of inhibition at 500µg/ml and 250µg/ml concentration respectively.

Biosynthesis of selenium nanoparticles by Aspergillus flavus and Candida albicans and comparison of their effects with antifungal drugs

2021 ◽  
Author(s):  
Mahdi Hosseini Bafghi ◽  
Razieh Nazari ◽  
Majid Darroudi ◽  
Mohsen Zargar ◽  
Hossein Zarrinfar
Keyword(s):  
Candida Albicans ◽  
Aspergillus Flavus ◽  
Fungal Pathogens ◽  
Chemical Properties ◽  
Cost Effective ◽  
Antifungal Drugs ◽  
Selenium Nanoparticles ◽  
Fungal Strains ◽  
Vis Spectroscopy ◽  
Physical And Chemical

Abstract Biosynthesis of nanoparticles can stand as a replacement for the available chemical and physical methods by offering new procedures as green syntheses that have proved to be simple, biocompatible, safe, and cost-effective. Considering how nanoparticles with a size of 1 to 100 nanometers contain unique physical and chemical properties, recent reports are indicative of observing the antifungal qualities of selenium nanoparticles (Se-NPs). Recently, the observance of antifungal resistance towards different species of these fungi is often reported. Therefore, due to the antifungal effects of biological nanoparticles, this study aimed to investigate the exertion of these nanoparticles and evaluate their effects on the growth of fungal pathogens. Se-NPs were biosynthesized by the application of wet reduction method, which included specific concentrations of Aspergillus flavus and Candida albicans. The presence of nanoparticles was confirmed by methods such as UV-Vis spectroscopy, FT-IR analysis, and FESEM electron microscope that involved FESEM and EDAX diagram. The fungal strains were cultured in sabouraud dextrose agar medium to perform the sensitivity test based on the minimum inhibitory concentration (MIC) method in duplicate. The utilization of Se-NPs at concentrations of 1 µg/ ml and below resulted in zero growth of fungal agents. However, their growth was inhibited by antifungal drugs at concentrations of 2 µg/ ml and higher. Based on the obtained results, biological nanoparticles produced by fungal agents at different concentrations exhibited favorable inhibitory effects on the growth of fungal strains.

scholarly journals Blockchain technology in maritime industry

Pomorstvo ◽  
2020 ◽  
Vol 34 (1) ◽  
pp. 178-184
Author(s):  
Ivan Peronja ◽  
Kristijan Lenac ◽  
Roko Glavinović
Keyword(s):  
Comparative Method ◽  
Maritime Industry ◽  
Comprehensive Overview ◽  
Time Value ◽  
Bill Of Lading ◽  
Blockchain Technology ◽  
The World ◽  
Transportation Process ◽  
Potential Impact ◽  
World Environment

Maritime industry is one of the most globally connected industries that include transportation of numerous types of goods and documents across the world. With that said, it is safe to say that abundance of financial and paper-trail transactions are made every day in order for goods to be transported from one place to another. The scope of this paper is to show that by implementing blockchain technology savings in time and money could be generated. This paper presents costs of container freights and rates in the last few years and assumes possible future costs of container freights and rates if blockchain based technology is implemented. Additionally, by using comparative method economical and time value of “traditional” bill of lading is compared with a blockchain bill of lading solution. It is also important to mention the potential impact of the blockchain technology on the world environment and ecology by reducing global paper consumption and emissions from vehicles that are used in the transportation process. This paper also gives a descriptive and comprehensive overview of current and future applications of blockchain technology in maritime industry.

scholarly journals When Researchers Embrace an Artistic Lens: A Review of Patricia Leavy’s Method Meets Art

2016 ◽  
Author(s):  
Matilda Mettälä
Keyword(s):  
Ways Of Knowing ◽  
Comprehensive Overview ◽  
The Arts ◽  
The World ◽  
Everyday Realities

Method Meets Art offers an enhanced view on how the artistic lens can provide new ways of knowing and become a source of deep enrichment in science; a means to understand everyday realities and the world. It serves as a methods book to all arts-based researchers coming from different disciplines as it includes a comprehensive overview with practical variations and research examples. It may also be of interest to researchers and artists outside the qualitative community from various fields as well as to anyone who wishes to explore the merging of science and the arts.

scholarly journals Novel Antifungal Compounds Discovered in Medicines for Malaria Venture’s Malaria Box

mSphere ◽  
2018 ◽  
Vol 3 (2) ◽  
Author(s):  
Eric H. Jung ◽  
David J. Meyers ◽  
Jürgen Bosch ◽  
Arturo Casadevall
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Cryptococcus Neoformans ◽  
Fungal Pathogens ◽  
Pathogenic Fungi ◽  
Cryptococcus Gattii ◽  
Antifungal Drugs ◽  
Resistant Bacteria ◽  
Animal Cells ◽  
Malaria Box

ABSTRACTSimilarities in fungal and animal cells make antifungal discovery efforts more difficult than those for other classes of antimicrobial drugs. Currently, there are only three major classes of antifungal drugs used for the treatment of systemic fungal diseases: polyenes, azoles, and echinocandins. Even in situations where the offending fungal organism is susceptible to the available drugs, treatment courses can be lengthy and unsatisfactory, since eradication of infection is often very difficult, especially in individuals with impaired immunity. Consequently, there is a need for new and more effective antifungal drugs. We have identified compounds with significant antifungal activity in the Malaria Box (Medicines for Malaria Ventures, Geneva, Switzerland) that have higher efficacy than some of the currently used antifungal drugs. Our best candidate, MMV665943 (IUPAC name 4-[6-[[2-(4-aminophenyl)-3H-benzimidazol-5-yl]methyl]-1H-benzimidazol-2-yl]aniline), here referred to as DM262, showed 16- to 32-fold-higher activity than fluconazole againstCryptococcus neoformans. There was also significant antifungal activity in other fungal species with known antifungal resistance, such asLomentospora prolificansandCryptococcus gattii. Antifungal activity was also observed against a common fungus,Candida albicans. These results are important because they offer a potentially new class of antifungal drugs and the repurposing of currently available therapeutics.IMPORTANCEMuch like the recent increase in drug-resistant bacteria, there is a rise in antifungal-resistant strains of pathogenic fungi. There is a need for novel and more potent antifungal therapeutics. Consequently, we investigated a mixed library of drug-like and probe-like compounds with activity inPlasmodiumspp. for activity against two common fungal pathogens,Cryptococcus neoformansandCandida albicans, along with two less common pathogenic species,Lomentospora prolificansandCryptococcus gattii. We uncover a previously uncharacterized drug with higher broad-spectrum antifungal activity than some current treatments. Our findings may eventually lead to a compound added to the arsenal of antifungal therapeutics.

Event Detection in Wireless Sensor Networks

2012 ◽  
pp. 226-238
Author(s):  
Sohail Anwar ◽  
Chongming Zhang
Keyword(s):  
Wireless Sensor Networks ◽  
Wireless Networks ◽  
Sensor Networks ◽  
Data Collection ◽  
Event Detection ◽  
Wireless Sensor ◽  
Comprehensive Overview ◽  
Detection Mechanism ◽  
Detection Techniques ◽  
The World

Wireless Sensor Networks (WSNs) have experienced an amazing evolution during the last decade. Compared with other wired or wireless networks, wireless sensor networks extend the range of data collection and make it possible for us to get information from every corner of the world. The chapter begins with an introduction to WSNs and their applications. The chapter recognizes event detection as a key component for WSN applications. The chapter provides a structured and comprehensive overview of various techniques used for event detection in WSNs. Existing event detection techniques have been grouped into threshold based and pattern based mechanisms. For each category of event detection mechanism, the chapter surveys some representative technical schemes. The chapter also provides some analyses on the relative strengths and weaknesses of these technical schemes. Towards the end, the trends in the research regarding the event detection in WSNs are described.

scholarly journals The importance of rapid diagnosis for multidrug-resistant Candida: an interview with Maurizio Sanguinetti

2019 ◽  
Vol 14 (12) ◽  
pp. 1011-1012
Author(s):  
Maurizio Sanguinetti
Keyword(s):  
Infectious Diseases ◽  
Fungal Pathogens ◽  
Fungal Infections ◽  
Resistance Mechanisms ◽  
Rapid Diagnosis ◽  
Antifungal Drugs ◽  
Full Professor ◽  
Research Activity ◽  
Diagnostic Strategies ◽  
Personalized Care

In this exclusive interview, Maurizio Sanguinetti discusses current issues with Candida fungal infection diagnoses, in light of its rising resistance to antifungal drugs. This interview was conducted by Ellen Colvin, Editor of Future Microbiology. Maurizio Sanguinetti, MD, is full Professor of Microbiology at the Università Cattolica del Sacro Cuore of Rome, Italy, and Director of the Institute of Microbiology and Chief of the Department of Laboratory Sciences and Infectious Diseases Sciences at the Fondazione Policlinico Agostino Gemelli IRCCS of Rome, Italy. For several years, the research activity of Maurizio Sanguinetti has mainly focused on the development of molecular methods for the rapid diagnosis of bacterial, mycobacterial and fungal infections; the elucidation of virulence and antimicrobial resistance mechanisms in clinically relevant bacterial and fungal pathogens; the characterization of the human microbiota in relationship to infectious and noninfectious diseases and implementation of new diagnostic strategies for the personalized care of patients with infectious diseases.

scholarly journals The Silent Killer: Consequences of Climate Change and How to Survive Past the Year 2050

2020 ◽  
Vol 12 (9) ◽  
pp. 3757
Author(s):  
Anna Laura Huckelba ◽  
Paul A. M. Van Lange
Keyword(s):  
Climate Change ◽  
Carbon Dioxide ◽  
Behavioral Change ◽  
Social Dilemma ◽  
Psychological Perspective ◽  
Short Term ◽  
Comprehensive Overview ◽  
Psychological Mechanisms ◽  
Self Interest ◽  
The World

There is strong scientific consensus that the climate is drastically changing due to increasing levels of carbon dioxide in the atmosphere, and that these changes are largely due to human behavior. Scientific estimates posit that by 2050, we will begin to experience some of the most damaging consequences of climate change, which will only worsen as the world becomes more populated and resources become scarcer. Considerable progress has been made to explore technological solutions, yet useful insights from a psychological perspective are still lacking. Understanding whether and how individuals and groups cope with environmental dilemmas is the first step to combatting climate change. The key challenge is how can we reduce a tendency to inaction and to understand the psychological obstacles for behavioral change that reduce climate change. We provide a social dilemma analysis of climate change, emphasizing three important ingredients: people need to recognize their own impact on the climate, there is conflict between self-interest and collective interests, and there is a temporal dilemma involving a conflict between short-term and longer-term interest. Acknowledging these features, we provide a comprehensive overview of psychological mechanisms that support inaction, and close by discussing potential solutions. In particular, we offer recommendations at the level of individuals, communities, and governments.

scholarly journals High Efficiency Drug Repurposing Design for New Antifungal Agents

2019 ◽  
Vol 2 (2) ◽  
pp. 31 ◽  
Author(s):  
Jong H. Kim ◽  
Kathleen L. Chan ◽  
Luisa W. Cheng ◽  
Lisa A. Tell ◽  
Barbara A. Byrne ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Fungal Pathogens ◽  
Antifungal Agents ◽  
High Efficiency ◽  
Intervention Strategy ◽  
Drug Repurposing ◽  
Antifungal Drugs ◽  
Antifungal Drug ◽  
Alternative Intervention ◽  
Combined Application

Current antifungal interventions have often limited efficiency in treating fungal pathogens, particularly those resistant to commercial drugs or fungicides. Antifungal drug repurposing is an alternative intervention strategy, whereby new utility of various marketed, non-antifungal drugs could be repositioned as novel antifungal agents. In this study, we investigated “chemosensitization” as a method to improve the efficiency of antifungal drug repurposing, wherein combined application of a second compound (viz., chemosensitizer) with a conventional, non-antifungal drug could greatly enhance the antifungal activity of the co-applied drug. Redox-active natural compounds or structural derivatives, such as thymol (2-isopropyl-5-methylphenol), 4-isopropyl-3-methylphenol, or 3,5-dimethoxybenzaldehyde, could serve as potent chemosensitizers to enhance antifungal activity of the repurposed drug bithionol. Of note, inclusion of fungal mutants, such as antioxidant mutants, could also facilitate drug repurposing efficiency, which is reflected in the enhancement of antifungal efficacy of bithionol. Bithionol overcame antifungal (viz., fludioxonil) tolerance of the antioxidant mutants of the human/animal pathogen Aspergillus fumigatus. Altogether, our strategy can lead to the development of a high efficiency drug repurposing design, which enhances the susceptibility of pathogens to drugs, reduces time and costs for new antifungal development, and abates drug or fungicide resistance.

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