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  1. Article ; Online: Open science approaches to COVID-19.

    Tse, Edwin G / Klug, Dana M / Todd, Matthew H

    F1000Research

    2020  Volume 9, Page(s) 1043

    Abstract: In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers ... ...

    Abstract In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers have adopted open science methods to begin to combat this disease
    MeSH term(s) Betacoronavirus ; Biomedical Research/trends ; COVID-19 ; Coronavirus Infections ; Humans ; Information Dissemination/methods ; Open Access Publishing/trends ; Pandemics ; Pneumonia, Viral ; SARS-CoV-2
    Keywords covid19
    Language English
    Publishing date 2020-08-25
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2699932-8
    ISSN 2046-1402 ; 2046-1402
    ISSN (online) 2046-1402
    ISSN 2046-1402
    DOI 10.12688/f1000research.26084.1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: tele

    Korsik, Marat / Tse, Edwin G / Smith, David G / Lewis, William / Rutledge, Peter J / Todd, Matthew H

    The Journal of organic chemistry

    2020  Volume 85, Issue 21, Page(s) 13438–13452

    Abstract: We have discovered and studied ... ...

    Abstract We have discovered and studied a
    MeSH term(s) Antimalarials/pharmacology ; Halogens ; Pyrazines ; Solvents
    Chemical Substances Antimalarials ; Halogens ; Pyrazines ; Solvents
    Language English
    Publishing date 2020-10-13
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.0c01045
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4473: Show issues Location:
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  3. Article ; Online: The past, present and future of anti-malarial medicines.

    Tse, Edwin G / Korsik, Marat / Todd, Matthew H

    Malaria journal

    2019  Volume 18, Issue 1, Page(s) 93

    Abstract: Great progress has been made in recent years to reduce the high level of suffering caused by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria prevention and the use of artemisinin-based combination therapy (ACT) for ... ...

    Abstract Great progress has been made in recent years to reduce the high level of suffering caused by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria prevention and the use of artemisinin-based combination therapy (ACT) for malaria treatment have made a significant impact. Nevertheless, the development of resistance to the past and present anti-malarial drugs highlights the need for continued research to stay one step ahead. New drugs are needed, particularly those with new mechanisms of action. Here the range of anti-malarial medicines developed over the years are reviewed, beginning with the discovery of quinine in the early 1800s, through to modern day ACT and the recently-approved tafenoquine. A number of new potential anti-malarial drugs currently in development are outlined, along with a description of the hit to lead campaign from which it originated. Finally, promising novel mechanisms of action for these and future anti-malarial medicines are outlined.
    MeSH term(s) Antimalarials/pharmacology ; Humans ; Malaria/drug therapy
    Chemical Substances Antimalarials
    Language English
    Publishing date 2019-03-22
    Publishing country England
    Document type Journal Article ; Review
    ISSN 1475-2875
    ISSN (online) 1475-2875
    DOI 10.1186/s12936-019-2724-z
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Open science approaches to COVID-19 [version 1; peer review

    Edwin G. Tse / Dana M. Klug / Matthew H. Todd

    F1000Research, Vol

    2 approved]

    2020  Volume 9

    Abstract: In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers ... ...

    Abstract In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers have adopted open science methods to begin to combat this disease via global collaborative efforts. We summarise here some of those initiatives, and have created an updateable list to which others may be added. Though open science has previously been shown as an accelerator of biomedical research, the COVID-19 crisis has made openness seem the logical choice. Will openness persist in the discovery of new medicines, after the crisis has receded?
    Keywords Medicine ; R ; Science ; Q
    Language English
    Publishing date 2020-08-01T00:00:00Z
    Publisher F1000 Research Ltd
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

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  5. Article ; Online: The past, present and future of anti-malarial medicines

    Edwin G. Tse / Marat Korsik / Matthew H. Todd

    Malaria Journal, Vol 18, Iss 1, Pp 1-

    2019  Volume 21

    Abstract: Abstract Great progress has been made in recent years to reduce the high level of suffering caused by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria prevention and the use of artemisinin-based combination therapy ( ... ...

    Abstract Abstract Great progress has been made in recent years to reduce the high level of suffering caused by malaria worldwide. Notably, the use of insecticide-treated mosquito nets for malaria prevention and the use of artemisinin-based combination therapy (ACT) for malaria treatment have made a significant impact. Nevertheless, the development of resistance to the past and present anti-malarial drugs highlights the need for continued research to stay one step ahead. New drugs are needed, particularly those with new mechanisms of action. Here the range of anti-malarial medicines developed over the years are reviewed, beginning with the discovery of quinine in the early 1800s, through to modern day ACT and the recently-approved tafenoquine. A number of new potential anti-malarial drugs currently in development are outlined, along with a description of the hit to lead campaign from which it originated. Finally, promising novel mechanisms of action for these and future anti-malarial medicines are outlined.
    Keywords Malaria ; Plasmodium ; Mechanism of action ; Drug discovery ; Drug development ; Arctic medicine. Tropical medicine ; RC955-962 ; Infectious and parasitic diseases ; RC109-216
    Language English
    Publishing date 2019-03-01T00:00:00Z
    Publisher BMC
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

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  6. Article: Open science approaches to COVID-19

    Tse, Edwin G / Klug, Dana M / Todd, Matthew H

    F1000Res

    Abstract: In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers ... ...

    Abstract In only a matter of months, the coronavirus disease of 2019 (COVID-19) has spread around the world. The global impact of the disease has caused significant and repeated calls for quick action towards new medicines and vaccines. In response, researchers have adopted open science methods to begin to combat this disease via global collaborative efforts. We summarise here some of those initiatives, and have created an updateable list to which others may be added. Though open science has previously been shown as an accelerator of biomedical research, the COVID-19 crisis has made openness seem the logical choice. Will openness persist in the discovery of new medicines, after the crisis has receded?
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #916550
    Database COVID19

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  7. Article ; Online: Structure-Property Optimization of a Series of Imidazopyridines for Visceral Leishmaniasis.

    Dichiara, Maria / Simpson, Quillon J / Quotadamo, Antonio / Jalani, Hitesh B / Huang, Anson X / Millard, Caroline C / Klug, Dana M / Tse, Edwin G / Todd, Matthew H / Silva, Daniel Gedder / da Silva Emery, Flavio / Carlson, J Eric / Zheng, Shao-Liang / Vleminckx, Margot / Matheeussen, An / Caljon, Guy / Pollastri, Michael P / Sjö, Peter / Perry, Benjamin /
    Ferrins, Lori

    ACS infectious diseases

    2023  Volume 9, Issue 8, Page(s) 1470–1487

    Abstract: Leishmaniasis is a collection of diseases caused by more than ... ...

    Abstract Leishmaniasis is a collection of diseases caused by more than 20
    MeSH term(s) Humans ; Leishmaniasis, Visceral/drug therapy ; Leishmaniasis ; Leishmania ; Neglected Diseases ; Imidazoles/pharmacology
    Chemical Substances imidazopyridine ; Imidazoles
    Language English
    Publishing date 2023-07-07
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S. ; Research Support, Non-U.S. Gov't
    ISSN 2373-8227
    ISSN (online) 2373-8227
    DOI 10.1021/acsinfecdis.3c00040
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: tele-Substitution Reactions in the Synthesis of a Promising Class of 1,2,4-Triazolo[4,3-a]pyrazine-Based Antimalarials

    Korsik, Marat / Tse, Edwin G. / Smith, David G. / Lewis, William / Rutledge, Peter J. / Todd, Matthew H.

    Journal of organic chemistry. 2020 Aug. 13, v. 85, no. 21

    2020  

    Abstract: We have discovered and studied a tele-substitution reaction in a biologically important heterocyclic ring system. Conditions that favor the tele-substitution pathway were identified: the use of increased equivalents of the nucleophile or decreased ... ...

    Abstract We have discovered and studied a tele-substitution reaction in a biologically important heterocyclic ring system. Conditions that favor the tele-substitution pathway were identified: the use of increased equivalents of the nucleophile or decreased equivalents of base or the use of softer nucleophiles, less polar solvents, and larger halogens on the electrophile. Using results from X-ray crystallographic and isotope labeling experiments, a mechanism for this unusual transformation is proposed. We focused on this triazolopyrazine as it is the core structure of the in vivo active antiplasmodium compounds of Series 4 of the Open Source Malaria consortium.
    Keywords Lewis acids ; Lewis bases ; X-ray diffraction ; antimalarials ; isotopes ; malaria ; organic chemistry
    Language English
    Dates of publication 2020-0813
    Size p. 13438-13452.
    Publishing place American Chemical Society
    Document type Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.0c01045
    Database NAL-Catalogue (AGRICOLA)

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    In stock of ZB MED Bonn / Germany

    Z 4' 49/42: Show issues
    Z 7.1: Show issues

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  9. Article: Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities.

    Munawar, Saba / Windley, Monique J / Tse, Edwin G / Todd, Matthew H / Hill, Adam P / Vandenberg, Jamie I / Jabeen, Ishrat

    Frontiers in pharmacology

    2018  Volume 9, Page(s) 1035

    Abstract: The hERG (human ether-a-go-go-related gene) encoded potassium ion ( ... ...

    Abstract The hERG (human ether-a-go-go-related gene) encoded potassium ion (K
    Language English
    Publishing date 2018-09-19
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2018.01035
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials.

    Tse, Edwin G / Houston, Sevan D / Williams, Craig M / Savage, G Paul / Rendina, Louis M / Hallyburton, Irene / Anderson, Mark / Sharma, Raman / Walker, Gregory S / Obach, R Scott / Todd, Matthew H

    Journal of medicinal chemistry

    2020  Volume 63, Issue 20, Page(s) 11585–11601

    Abstract: The replacement of one chemical motif with another that is broadly similar is a common method in medicinal chemistry to modulate the physical and biological properties of a molecule (i.e., bioisosterism). In recent years, bioisosteres such as cubane and ... ...

    Abstract The replacement of one chemical motif with another that is broadly similar is a common method in medicinal chemistry to modulate the physical and biological properties of a molecule (i.e., bioisosterism). In recent years, bioisosteres such as cubane and bicyclo[1.1.1]pentane (BCP) have been used as highly effective phenyl mimics. Herein, we show the successful incorporation of a range of phenyl bioisosteres during the open-source optimization of an antimalarial series. Cubane (
    MeSH term(s) Antimalarials/chemical synthesis ; Antimalarials/chemistry ; Antimalarials/pharmacology ; Antimalarials/toxicity ; Boron Compounds/chemistry ; Bridged Bicyclo Compounds/chemical synthesis ; Bridged Bicyclo Compounds/chemistry ; Bridged Bicyclo Compounds/pharmacology ; Bridged Bicyclo Compounds/toxicity ; Cell Survival/drug effects ; Chemistry, Pharmaceutical ; Drug Design ; Hep G2 Cells ; Humans ; Molecular Structure ; Plasmodium falciparum/drug effects
    Chemical Substances Antimalarials ; Boron Compounds ; Bridged Bicyclo Compounds
    Language English
    Publishing date 2020-09-30
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c00746
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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    Zs.MB 1: Show issues

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