Antifungal Compounds Discovery

Antifungal Compounds Discovery
Author: Marina Sokovic,Konstantinos Liaras
Publsiher: Elsevier
Total Pages: 300
Release: 2020-09-15
ISBN 10: 9780128158241
ISBN 13: 0128158247
Language: EN, FR, DE, ES & NL

Antifungal Compounds Discovery Book Review:

Fungi are both the cause of many major health problems and an incredible source of compounds for developing new medicinal treatments, and with the increasing emergence of multidrug resistance, the need for new antimicrobial agents is greater than ever. Antifungal Compound Discovery provides researchers with a detailed study of both natural and synthetic compounds that can be effective against a variety of fungal species, supporting and encouraging the design of innovative, potent new drug candidates for the treatment of fungal infections. Beginning with an introduction to both the history and latest developments in this field, the book goes on to provide helpful background information on key fungal species before outlining current antifungal therapies and reasons further development is needed. Detailed chapters then follow reviewing a broad range of natural and synthetic antifungal agents, and discussing the synergistic effect of working with both simultaneously. Finally, the book concludes by considering potential future developments in this important field. Supported with detailed schemes and key information on the biological activity of all selected compounds, Antifungal Compound Discovery is a comprehensive guide helping researchers understand the relationship between specific chemicals structures and their antifungal potency, and a key tool for all those involved in the identification and development of antimicrobial compounds. Provides an overview of the most specific mycotic infections and fungal species as background for compound development Presents the chemical formulas of all natural and synthetic compounds reviewed Combines detailed information about origin, isolation and possible therapeutic uses of all indexed compounds, including biological activity, mechanism of action and SAR information

Antifungal Compounds Discovery development and uses

Antifungal Compounds  Discovery  development  and uses
Author: Malcolm R. Siegel,Hugh Delane Sisler
Publsiher: Unknown
Total Pages: 1274
Release: 1977-01-01
ISBN 10: 9780824765576
ISBN 13: 0824765575
Language: EN, FR, DE, ES & NL

Antifungal Compounds Discovery development and uses Book Review:

V. 1- Discovery, developments, and uses; v. 2 - Interactions in biological and ecological systems.

Antifungal Compounds Discovery

Antifungal Compounds Discovery
Author: Marina Sokovic,Konstantinos Liaras
Publsiher: Elsevier
Total Pages: 290
Release: 2020-09-30
ISBN 10: 0128158255
ISBN 13: 9780128158258
Language: EN, FR, DE, ES & NL

Antifungal Compounds Discovery Book Review:

Fungi are both the cause of many major health problems and an incredible source of compounds for developing new medicinal treatments, and with the increasing emergence of multidrug resistance, the need for new antimicrobial agents is greater than ever. Antifungal Compound Discovery provides researchers with a detailed study of both natural and synthetic compounds that can be effective against a variety of fungal species, supporting and encouraging the design of innovative, potent new drug candidates for the treatment of fungal infections. Beginning with an introduction to both the history and latest developments in this field, the book goes on to provide helpful background information on key fungal species before outlining current antifungal therapies and reasons further development is needed. Detailed chapters then follow reviewing a broad range of natural and synthetic antifungal agents, and discussing the synergistic effect of working with both simultaneously. Finally, the book concludes by considering potential future developments in this important field. Supported with detailed schemes and key information on the biological activity of all selected compounds, Antifungal Compound Discovery is a comprehensive guide helping researchers understand the relationship between specific chemicals structures and their antifungal potency, and a key tool for all those involved in the identification and development of antimicrobial compounds. Provides an overview of the most specific mycotic infections and fungal species as background for compound development Presents the chemical formulas of all natural and synthetic compounds reviewed Combines detailed information about origin, isolation and possible therapeutic uses of all indexed compounds, including biological activity, mechanism of action and SAR information

Anti fungal Drug Discovery

Anti fungal Drug Discovery
Author: Bradley Mark Tebbets
Publsiher: Unknown
Total Pages: 208
Release: 2012
ISBN 10: 1928374650XXX
ISBN 13: OCLC:822841247
Language: EN, FR, DE, ES & NL

Anti fungal Drug Discovery Book Review:

Discovery Identification and Evaluation of Antifungal Compounds Produced by Pseudomonas Syringae

Discovery  Identification  and Evaluation of Antifungal Compounds Produced by Pseudomonas Syringae
Author: Kevin N. Sorensen
Publsiher: Unknown
Total Pages: 238
Release: 1997
ISBN 10: 1928374650XXX
ISBN 13: OCLC:43961652
Language: EN, FR, DE, ES & NL

Discovery Identification and Evaluation of Antifungal Compounds Produced by Pseudomonas Syringae Book Review:

Antifungal Drug Discovery New Theories and New Therapies

Antifungal Drug Discovery  New Theories and New Therapies
Author: Chaminda Jayampath Seneviratne,Edvaldo Antonio Ribeiro Rosa
Publsiher: Frontiers Media SA
Total Pages: 135
Release: 2016-09-13
ISBN 10: 2889199509
ISBN 13: 9782889199501
Language: EN, FR, DE, ES & NL

Antifungal Drug Discovery New Theories and New Therapies Book Review:

Fungal infections such as candidoses can range from superficial mucous membrane infection to life-threatening systemic mycoses. Candida infections are a significant clinical problem globally due to rapid rise in compromised host populations including HIV/AIDS, organ transplant recipients and patients on chemotherapy. In addition, sharp increase in aging populations which are susceptible to fungal infections is expected in next few decades. Antifungal drugs are relatively difficult to develop compared to the antibacterial drugs owing to the eukaryotic nature of the cells. Therefore, only a handful of antifungal agents are currently available to treat the myriad of fungal infections. Moreover, rising antifungal resistance and host-related adverse reactions have limited the antifungal arsenal against fungal pathogens. In this research topic, we tried to update the theoretical aspects pertaining to the antifungal drug discovery i.e. proposed novel mechanisms, new drug targets and pathways. In addition, invited authors explored the new antifungal drugs derived from natural and synthetic sources which are currently under development. Contributors were encouraged to bring new insight into the antifungal drug discovery. We hope the reader may arrive at a general consensus on the possible strategies to combat ever increasing ubiquitous fungal infection in this new century.

Discovery Purification and Characterization of Antifungal Proteins and Other Defense related Compounds from Tropical Plants

Discovery  Purification and Characterization of Antifungal Proteins and Other Defense related Compounds from Tropical Plants
Author: Tahzeeba Hossain
Publsiher: Unknown
Total Pages: 872
Release: 1999
ISBN 10: 1928374650XXX
ISBN 13: OCLC:48593616
Language: EN, FR, DE, ES & NL

Discovery Purification and Characterization of Antifungal Proteins and Other Defense related Compounds from Tropical Plants Book Review:

Antifungal Agents

Antifungal Agents
Author: G. K. Dixon,Leonard G. Copping,Derek W. Hollomon
Publsiher: Bios Scientific Pub Limited
Total Pages: 292
Release: 1995
ISBN 10: 1928374650XXX
ISBN 13: UCSC:32106012733215
Language: EN, FR, DE, ES & NL

Antifungal Agents Book Review:

Explores how new molecular technologies are interfacing with chemistry and biology in the search for new fungicide targets.

Antimicrobial Drug Discovery

Antimicrobial Drug Discovery
Author: George Tegos,Eleftherios Mylonakis
Publsiher: CABI
Total Pages: 357
Release: 2012
ISBN 10: 1845939433
ISBN 13: 9781845939434
Language: EN, FR, DE, ES & NL

Antimicrobial Drug Discovery Book Review:

Resistance is on the rise among a variety of human pathogenic microorganisms associated with common and potentially life-threatening infections, including penicillin-resistant Streptococcus pneumonia and Methicillin-resistant Staphylococcus aureus (MRSA). There is increasing demand to approach the threat of multidrug resistance incorporating novel multidisciplinary methodologies and technological platforms. This book documents the latest research, covering current and promising activities in four key areas: computational chemistry and chemoinformatics, High Throughput Screening (HTS), non-vertebrate model hosts and light and nano-based technologies. It is essential reading for researchers and students in microbiology, biotechnology, pharmacology, chemistry and biology as well as medical professionals.

Impedance Based De Replication Of Antifungal Drug Classes

Impedance Based De Replication Of Antifungal Drug Classes
Author: J. Wuyts
Publsiher: Unknown
Total Pages: 135
Release: 2017
ISBN 10: 1928374650XXX
ISBN 13: OCLC:1250395727
Language: EN, FR, DE, ES & NL

Impedance Based De Replication Of Antifungal Drug Classes Book Review:

Impedance-based de-replication of antifungal drug classes High-throughput target-based drug screening of synthetic molecules so far has not resulted in new antifungal drug classes. One of the proposed reasons for this failure is the lack of penetration of synthetic molecules in the fungal cell, the high false-positive rates and the lack of selectivity. Three major classes of antifungal drugs are currently in use; the polyenes, the echinocandins and the azoles. Two of them, the polyenes and the echinocandins, are natural products or based on natural products produced by micro-organisms. Small molecules produced by micro-organisms have several desirable characteristics. First, they are highly specific due to their high degree of chirality. Second, they are intrinsically cell permeable and finally, they occupy a more diverse chemical space. However, natural product-based antifungal drug discovery is associated with a number of technical challenges. Fermentation extracts are composed of complex mixtures containing hundreds or thousands of unknown compounds and concomitantly natural product drug discovery is plagued by a high background of known and/or nuisance compounds. Recent efforts have revealed that the vast majority of micro-organisms are still unable to grow under laboratory conditions, indicating a huge unexplored source of new natural compounds. Mining this so-called u2018microbial dark matteru2019 has recently proven successful in the search for novel antibiotics, but has not been used in the search for novel antifungals. Even though previously uncultured micro-organisms can be a rich source of novel antimicrobials, they still produce known antimicrobials. Therefore, a high-throughput de-replication platform to filter out known or undesirable compounds would decrease costs and time consumption in antifungal drug discovery. We have developed a novel tool that can be used to de-replicate antifungal drug classes in a high-throughput and label-free fashion. This tool is based on multisine electrochemical impedance spectroscopy (EIS). Here, Candida albicans biofilms were grown on modified microtiter plates with gold electrodes coated at the bottom of the plates. Next, the cells were subjected to a small alternating potential inside the wells of the 96 well plates during biofilm development or destruction for 24h. The measurement of the resulting micro-current through the developing biofilm results in a signature profile based on multiple frequency components. When we challenged growing C. albicans biofilms with different antifungals we were able to obtain specific signatures for each class. By comparing the signature profile of unknown compounds with a library of signature profiles of known compounds we were able to identify the antifungal mode-of-action. Impedance based de-replication can become a valuable tool in the next-generation of natural product-based drug discovery platforms.

7

7
Author: J. Wuyts
Publsiher: Unknown
Total Pages: 135
Release: 2017
ISBN 10: 1928374650XXX
ISBN 13: OCLC:1163813559
Language: EN, FR, DE, ES & NL

7 Book Review:

Impedance-based de-replication of antifungal drug classes High-throughput target-based drug screening of synthetic molecules so far has not resulted in new antifungal drug classes. One of the proposed reasons for this failure is the lack of penetration of synthetic molecules in the fungal cell, the high false-positive rates and the lack of selectivity. Three major classes of antifungal drugs are currently in use; the polyenes, the echinocandins and the azoles. Two of them, the polyenes and the echinocandins, are natural products or based on natural products produced by micro-organisms. Small molecules produced by micro-organisms have several desirable characteristics. First, they are highly specific due to their high degree of chirality. Second, they are intrinsically cell permeable and finally, they occupy a more diverse chemical space. However, natural product-based antifungal drug discovery is associated with a number of technical challenges. Fermentation extracts are composed of complex mixtures containing hundreds or thousands of unknown compounds and concomitantly natural product drug discovery is plagued by a high background of known and/or nuisance compounds. Recent efforts have revealed that the vast majority of micro-organisms are still unable to grow under laboratory conditions, indicating a huge unexplored source of new natural compounds. Mining this so-called u2018microbial dark matteru2019 has recently proven successful in the search for novel antibiotics, but has not been used in the search for novel antifungals. Even though previously uncultured micro-organisms can be a rich source of novel antimicrobials, they still produce known antimicrobials. Therefore, a high-throughput de-replication platform to filter out known or undesirable compounds would decrease costs and time consumption in antifungal drug discovery. We have developed a novel tool that can be used to de-replicate antifungal drug classes in a high-throughput and label-free fashion. This tool is based on multisine electrochemical impedance spectroscopy (EIS). Here, Candida albicans biofilms were grown on modified microtiter plates with gold electrodes coated at the bottom of the plates. Next, the cells were subjected to a small alternating potential inside the wells of the 96 well plates during biofilm development or destruction for 24h. The measurement of the resulting micro-current through the developing biofilm results in a signature profile based on multiple frequency components. When we challenged growing C. albicans biofilms with different antifungals we were able to obtain specific signatures for each class. By comparing the signature profile of unknown compounds with a library of signature profiles of known compounds we were able to identify the antifungal mode-of-action. Impedance based de-replication can become a valuable tool in the next-generation of natural product-based drug discovery platforms.

Antifungal Compounds

Antifungal Compounds
Author: Malcolm Richard Siegel,Hugh Delane Sisler
Publsiher: Unknown
Total Pages: 600
Release: 1977
ISBN 10: 1928374650XXX
ISBN 13: OCLC:37949942
Language: EN, FR, DE, ES & NL

Antifungal Compounds Book Review:

Antifungal Therapy

Antifungal Therapy
Author: Mahmoud A. Ghannoum, PhD, EMBA,Mahmoud A. Ghannoum,John R. Perfect,John R. Perfect, MD
Publsiher: CRC Press
Total Pages: 488
Release: 2016-04-19
ISBN 10: 0849387868
ISBN 13: 9780849387869
Language: EN, FR, DE, ES & NL

Antifungal Therapy Book Review:

A concise one-stop-practical reference for the various physicians dealing with fungal infections, Antifungal Therapy appeals to infectious disease physicians, transplant surgeons, dermatologists, and intensivists, as well as basic scientists and pharmaceutical company researchers interested in the state of antifungal therapy. This book provides a comprehensive, up-to-date overview of the pertinent issues pertaining to antifungal treatment. Divided into four interrelated sections for a cohesive discussion covers: history of antifungals from the discovery of the polyenes to the echinocandins antifungal susceptibility methods patient management animal models in drug development therapeutic strategies pharmacokinetic and pharmacogenomics trends in resistance

Insights in the Biosynthesis of Griseofulvin and Echinocandin B Two Antifungal Compounds from Ascomycetes

Insights in the Biosynthesis of Griseofulvin and Echinocandin B  Two Antifungal Compounds from Ascomycetes
Author: Ralph Adrian Cacho
Publsiher: Unknown
Total Pages: 218
Release: 2015
ISBN 10: 1928374650XXX
ISBN 13: OCLC:924398314
Language: EN, FR, DE, ES & NL

Insights in the Biosynthesis of Griseofulvin and Echinocandin B Two Antifungal Compounds from Ascomycetes Book Review:

Natural products, since the discovery of the first antibiotic penicillin in 1928, have been the source of and inspiration for drugs. Due the emergence of drug-resistant pathogens and discovery of drug targets in cancer biology, the need for the discovery of new bioactive natural compounds and synthesis of analogs thereof remains present. Fortuitously, the development of next-generation sequencing and tools for the heterologous expression of the biosynthetic genes for natural products has accelerated the discovery of new natural products as well as the elucidation of the respective biosynthetic pathways. This dissertation describes the use of these two emerging technologies in revealing insights in the biosynthesis of two antifungal natural compounds synthesized by filamentous fungi: griseofulvin, an antifungal drug used in treatment against dermatophytes and is in the World Health Organization List of Essential Medicine and echinocandin B, the parent compound of the frontline anti-Candidiasis drug anidulafungin. This dissertation will first present the work in the investigation the biosynthesis of echinocandin B. Invasive candidiasis caused by opportunistic pathogenic strains of genus Candida, accounts for 17% of ICU-related infections and through understanding of the biosynthesis of echinocandin B will aid in the mutasynthesis of analogs with better efficacy than the parent compound. In this work, we characterized the key steps in the biosynthesis of the natural product. Deletion of the biosynthetic genes also allowed for the mutasynthesis of echinocandin B analogs with more potent antifungal activity and showed the potential for re-engineering of the pathway to produce "unnatural" natural compounds. Moreover, this work also describes the full elucidation and reconstitution of the enzymatic reactions leading to the biosynthesis of griseofulvin using a combination of gene knockout and biochemical characterization of the griseofulvin biosynthetic enzymes. Among the important biosynthetic enzymes characterized in this study is the non-reducing polyketide synthase GsfA which was implicated in the biosynthesis of norlichexanthone and the cytochrome P450 GsfF which catalyzes the formation of the spirobicyclic grisan ring in griseofulvin. The culmination of this study is the demonstration of the total in vitro biosynthesis of the compound using purified griseofulvin biosynthetic enzymes.

Drug Design

Drug Design
Author: Arli Aditya Parikesit
Publsiher: BoD – Books on Demand
Total Pages: 158
Release: 2021-06-16
ISBN 10: 1789847524
ISBN 13: 9781789847529
Language: EN, FR, DE, ES & NL

Drug Design Book Review:

Right before the COVID-19 pandemic declared by the World Health Organization (WHO), life sciences have incited novel areas of studies that revolutionize the health sector. They are the studies of structural bioinformatics, pharmacogenomics, and metabolomics. The structural bioinformatics field is the very foundation of drug design research, as it provides insight into the molecular simulations and interactions between the biomolecules and the drug candidates. Secondly, pharmacogenomics is the starting point of any efforts in developing personalized medicine. Lastly, metabolomics provides instrumentation to elicit biomarkers for various diseases and health conditions. These studies have enabled current accelerated effort in COVID-19 research, as well as other communicable and non-communicable diseases.

Plant Bioactives and Drug Discovery

Plant Bioactives and Drug Discovery
Author: Valdir Cechinel-Filho
Publsiher: John Wiley & Sons
Total Pages: 586
Release: 2012-04-11
ISBN 10: 1118259920
ISBN 13: 9781118259924
Language: EN, FR, DE, ES & NL

Plant Bioactives and Drug Discovery Book Review:

An in-depth exploration of the applications of plant bioactive metabolites in drug research and development Highlighting the complexity and applications of plant bioactive metabolites in organic and medicinal chemistry, Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives provides an in-depth overview of the ways in which plants can inform drug research and development. An edited volume featuring multidisciplinary international contributions from acclaimed scientists researching bioactive natural products, the book provides an incisive overview of one of the most important topics in pharmaceutical studies today. With coverage of strategic methods of natural compound isolation, structural manipulation, natural products in clinical trials, quality control, and more, and featuring case studies on medicinal plants, the book serves as a definitive guide to the field of plant biodiversity as it relates to medicine. In addition, chapters on using natural products as drugs that target specific disease areas, including neurological disorders, inflammation, infectious diseases, and cancer, illustrate the myriad possibilities for therapeutic applications. Wide ranging and comprehensive, Plant Bioactives and Drug Discovery also includes important information on marketing, regulations, intellectual property rights, and academic-industry collaboration as they relate to plant-based drug research, making it an essential resource for advanced students and academic and industry professionals working in biochemical, pharmaceutical, and related fields.

Combating Fungal Infections

Combating Fungal Infections
Author: Iqbal Ahmad,Mohammad Owais,Mohammed Shahid,Farrukh Aqil
Publsiher: Springer Science & Business Media
Total Pages: 539
Release: 2010-08-03
ISBN 10: 9783642121739
ISBN 13: 364212173X
Language: EN, FR, DE, ES & NL

Combating Fungal Infections Book Review:

Fungi are eukaryotic microorganisms that are closely related to humans at cellular level. Human fungal pathogens belong to various classes of fungi, mainly zygo- cetes, ascomycetes, basidiomycetes, and deuteromycetes. In recent years, fungal infections have dramatically increased as a result of improved diagnosis, high frequency of catheterization, instrumentation, etc. However, the main cause remains the increasing number of immunosuppressed patients, mostly because of HIV infection and indiscriminate usage of antineoplastic and immunosuppressive agents, broad-spectrum antibiotics and prosthetic devices, and grafts in clinical settings. Presently available means of combating fungal infections are still weak and clumsy compared to control of bacterial infection. The present scenario of antifungal therapy is still based on two classes of antifungal drugs (polyenes and azoles). These drugs are effective in many cases, but display toxicity and limited spectrum of ef?cacy. The recent trend towards emergence of drug-resistant isolates in the clinic is an additional problem. In recent years, a few new antifungal drugs have entered the clinics, but they are expected to undergo same fate as the older antifungal drugs. The application of fungal genomics offers an unparalleled opportunity to develop novel antifungal drugs. However, it is too early to expect any novel drugs, as the antifungal drug discovery program is in the stage of infancy. Interestingly, several novel antifungal drug targets have been identi?ed and validated.

Plant Bioactives and Drug Discovery

Plant Bioactives and Drug Discovery
Author: Valdir Cechinel-Filho
Publsiher: John Wiley & Sons
Total Pages: 565
Release: 2012-05-22
ISBN 10: 047058226X
ISBN 13: 9780470582268
Language: EN, FR, DE, ES & NL

Plant Bioactives and Drug Discovery Book Review:

An in-depth exploration of the applications of plant bioactive metabolites in drug research and development Highlighting the complexity and applications of plant bioactive metabolites in organic and medicinal chemistry, Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives provides an in-depth overview of the ways in which plants can inform drug research and development. An edited volume featuring multidisciplinary international contributions from acclaimed scientists researching bioactive natural products, the book provides an incisive overview of one of the most important topics in pharmaceutical studies today. With coverage of strategic methods of natural compound isolation, structural manipulation, natural products in clinical trials, quality control, and more, and featuring case studies on medicinal plants, the book serves as a definitive guide to the field of plant biodiversity as it relates to medicine. In addition, chapters on using natural products as drugs that target specific disease areas, including neurological disorders, inflammation, infectious diseases, and cancer, illustrate the myriad possibilities for therapeutic applications. Wide ranging and comprehensive, Plant Bioactives and Drug Discovery also includes important information on marketing, regulations, intellectual property rights, and academic-industry collaboration as they relate to plant-based drug research, making it an essential resource for advanced students and academic and industry professionals working in biochemical, pharmaceutical, and related fields.

Recent Trends in the Discovery Development and Evaluation of Antifungal Agents

Recent Trends in the Discovery  Development and Evaluation of Antifungal Agents
Author: Robert A. Fromtling
Publsiher: Unknown
Total Pages: 641
Release: 1987
ISBN 10: 1928374650XXX
ISBN 13: UOM:39015035784159
Language: EN, FR, DE, ES & NL

Recent Trends in the Discovery Development and Evaluation of Antifungal Agents Book Review:

Preclinical Antimicrobial Drug Discovery

Preclinical Antimicrobial Drug Discovery
Author: Bill Lee
Publsiher: Unknown
Total Pages: 254
Release: 2006
ISBN 10: 1928374650XXX
ISBN 13: OCLC:253842059
Language: EN, FR, DE, ES & NL

Preclinical Antimicrobial Drug Discovery Book Review:

"The incidence of infections caused by antibiotic-resistant bacteria and fungi is rising rapidly. Once considered as little more than a nuisance, antibiotic resistance has become a serious threat. The mortality rate for some infections is approaching that of the pre-antibiotic era. New antimicrobials are needed urgently. Prior to the introduction of any new antimicrobial, comprehensive toxicity and efficacy profiles are assessed in preclinical studies. This thesis focuses on two key stages of preclinical antimicrobial drug development, specifically compound screening in vitro and animal efficacy testing in vivo. We developed a sensitive colorimetric platform with high-throughput capacity for the rapid screening of candidate antimicrobials. This platform could be adapted to assess compounds targeting a range of bacteria, fungi (such as Candida albicans), and protozoan parasites (such as Leishmania major). When this assay was modified to measure minimum inhibitory concentrations (MICs) for bacteria, 100% agreement within one dilution was achieved compared to the gold-standard method. A novel antifungal compound was taken forward to animal testing in an immunocompromised mouse model. We demonstrated herein that a histone deacetylase inhibitor in combination with an imidazole can synergise to produce a potent antifungal effect. A dose-dependent response, defined as a lower fungal burden and a higher survival rate, was achieved with increasing concentrations of the novel inhibitor." --