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  1. Article ; Online: Four decades of continuing innovations in the development of antiretroviral therapy for HIV/AIDS: Progress to date and future challenges.

    Ghosh, Arun K

    Global health & medicine

    2023  Volume 5, Issue 4, Page(s) 194–198

    Abstract: The treatment of HIV-1 infection and AIDS represents one of the greatest challenges in medicine. While there is no cure for HIV/AIDS, truly remarkable progress has been made for treatment of HIV/AIDS patients today. The advent of combination ... ...

    Abstract The treatment of HIV-1 infection and AIDS represents one of the greatest challenges in medicine. While there is no cure for HIV/AIDS, truly remarkable progress has been made for treatment of HIV/AIDS patients today. The advent of combination antiretroviral therapy (cART) in the mid-1990s dramatically improved HIV-1 related morbidity, greatly prolonged life expectancy, and delayed progression of AIDS. Due to current antiretroviral therapy, the mortality rate for HIV infected patients is closely approaching the mortality rate for the general population. The long-term success of HIV-AIDS treatment requires continued enhancement of cART with further development of novel drugs that would exhibit fewer side effects, higher genetic barrier to the development of resistance, and longer action with durable virologic suppression. This editorial article provides a quick review of four decades of intense drug development research efforts targeting various viral enzymes and cellular host factors leading to the evolution of today's treatment of patients with HIV-1 infection and AIDS. It also touches on challenges of future treatment options.
    Language English
    Publishing date 2023-08-31
    Publishing country Japan
    Document type Editorial
    ZDB-ID 3140544-7
    ISSN 2434-9194 ; 2434-9194 ; 2434-9186
    ISSN (online) 2434-9194
    ISSN 2434-9194 ; 2434-9186
    DOI 10.35772/ghm.2023.01013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Book: Aspartic acid proteases as therapeutic targets

    Ghosh, Arun K.

    (Methods and principles in medicinal chemistry ; 45)

    2010  

    Author's details ed. by Arun K. Ghosh
    Series title Methods and principles in medicinal chemistry ; 45
    Collection
    Keywords Aspartatproteasen ; Targeted drug delivery ; Arzneimittelentwicklung
    Subject Arzneimittel ; Drug Development ; Drug targeting ; Gezielte Pharmakotherapie ; Zielgerichtete Pharmakotherapie ; EC 3.4.23 ; Aspartatproteinasen ; Aspartylproteasen
    Language English
    Size XXIII, 615 S. : Ill., graph. Darst., 24 cm
    Publisher Wiley-VCH
    Publishing place Weinheim
    Publishing country Germany
    Document type Book
    HBZ-ID HT016514261
    ISBN 978-3-527-31811-7 ; 3-527-31811-9
    Database Catalogue ZB MED Medicine, Health

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    In stock of ZB MED Cologne/Königswinter

    Shelf markLoan statusLocation
    2010 A 4638 order for loan Magazin

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  3. Article: An Enzymatic Route to the Synthesis of Tricyclic Fused Hexahydrofuranofuran P2-Ligand for a Series of Highly Potent HIV-1 Protease Inhibitors.

    Ghosh, Arun K / Sharma, Ashish / Ghazi, Somayeh

    Tetrahedron letters

    2024  Volume 140

    Abstract: We describe a stereoselective synthesis of an optically active ( ... ...

    Abstract We describe a stereoselective synthesis of an optically active (1
    Language English
    Publishing date 2024-03-16
    Publishing country England
    Document type Journal Article
    ZDB-ID 204287-3
    ISSN 1873-3581 ; 0040-4039
    ISSN (online) 1873-3581
    ISSN 0040-4039
    DOI 10.1016/j.tetlet.2024.155013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Synthesis of optically active SARS-CoV-2 Mpro inhibitor drug nirmatrelvir (Paxlovid): an approved treatment of COVID-19.

    Ghosh, Arun K / Yadav, Monika

    Organic & biomolecular chemistry

    2023  Volume 21, Issue 28, Page(s) 5768–5774

    Abstract: Nirmatrelvir (Paxlovid) is an FDA approved drug that targets SARS-COV-2 3CLprotease. We report an optically active synthesis of nirmatrelvir that avoids a critical epimerization step. Our initial coupling ... ...

    Abstract Nirmatrelvir (Paxlovid) is an FDA approved drug that targets SARS-COV-2 3CLprotease. We report an optically active synthesis of nirmatrelvir that avoids a critical epimerization step. Our initial coupling of
    MeSH term(s) Humans ; SARS-CoV-2 ; COVID-19 ; Proline ; Antiviral Agents/pharmacology
    Chemical Substances nirmatrelvir and ritonavir drug combination ; Proline (9DLQ4CIU6V) ; Antiviral Agents
    Language English
    Publishing date 2023-07-19
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/d3ob00653k
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Total Synthesis of Neuroprotective Agents, (+)-Lycibarbarine A and (-)-Lycibarbarine B.

    Ghosh, Arun K / Harper, Marc / Robinson, William L

    The Journal of organic chemistry

    2023  Volume 88, Issue 13, Page(s) 9530–9536

    Abstract: We describe the convergent total syntheses of lycibarbarines A and B which are potent neuroprotective agents recently isolated from the fruits ... ...

    Abstract We describe the convergent total syntheses of lycibarbarines A and B which are potent neuroprotective agents recently isolated from the fruits of
    MeSH term(s) Neuroprotective Agents/pharmacology ; Alkylation ; Oxazines
    Chemical Substances Neuroprotective Agents ; Oxazines
    Language English
    Publishing date 2023-06-02
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; 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.3c00749
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Total Syntheses of the Proposed Structure of Iriomoteolide-1a, -1b and Synthesis of Three Derivatives for Structural Studies.

    Ghosh, Arun K / Yuan, Hao

    Marine drugs

    2022  Volume 20, Issue 10

    Abstract: Iriomoteolide-1a and iriomoteolide-1b are very potent cytotoxic agents, isolated from marine dinoflagellates. We carried out the enantioselective syntheses of the proposed structures of these natural products. However, our analysis of the NMR spectra of ... ...

    Abstract Iriomoteolide-1a and iriomoteolide-1b are very potent cytotoxic agents, isolated from marine dinoflagellates. We carried out the enantioselective syntheses of the proposed structures of these natural products. However, our analysis of the NMR spectra of the synthetic iriomoteolide-1a and the natural products revealed that the structures of iriomoteolide-1a and iriomoteolide-1b were assigned incorrectly. Based upon our detailed analysis of the spectral data of the synthetic iriomoteolide-1a and the natural products, we rationally designed three diastereomers of the proposed structure of
    MeSH term(s) Stereoisomerism ; Macrolides/pharmacology ; Macrolides/chemistry ; Biological Products/chemistry ; Cytotoxins ; Molecular Structure
    Chemical Substances iriomoteolide-1b ; iriomoteolide-1a ; Macrolides ; Biological Products ; Cytotoxins
    Language English
    Publishing date 2022-09-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2175190-0
    ISSN 1660-3397 ; 1660-3397
    ISSN (online) 1660-3397
    ISSN 1660-3397
    DOI 10.3390/md20100587
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

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  7. Article ; Online: Enantioselective Total Synthesis of (+)-EBC-23, a Potent Anticancer Agent from the Australian Rainforest.

    Ghosh, Arun K / Hsu, Che-Sheng

    The Journal of organic chemistry

    2021  Volume 86, Issue 9, Page(s) 6351–6360

    Abstract: We describe here an enantioselective synthesis of (+)-EBC-23, a potent anticancer agent from the Australian rainforest. Our convergent synthesis features a [3+2] dipolar cycloaddition of an olefin-bearing 1,3- ...

    Abstract We describe here an enantioselective synthesis of (+)-EBC-23, a potent anticancer agent from the Australian rainforest. Our convergent synthesis features a [3+2] dipolar cycloaddition of an olefin-bearing 1,3-
    MeSH term(s) Antineoplastic Agents ; Australia ; Pyrans ; Rainforest ; Spiro Compounds ; Stereoisomerism
    Chemical Substances Antineoplastic Agents ; EBC-23 ; Pyrans ; Spiro Compounds
    Language English
    Publishing date 2021-04-19
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.1c00172
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Highly Diastereoselective Intramolecular Asymmetric Oxidopyrylium-olefin [5 + 2] Cycloaddition and Synthesis of 8-Oxabicyclo[3.2.1]oct-3-enone Containing Ring Systems.

    Ghosh, Arun K / Yadav, Monika

    The Journal of organic chemistry

    2021  Volume 86, Issue 12, Page(s) 8127–8142

    Abstract: We have the investigated base mediated asymmetric intramolecular oxidopyrylium-alkene [5 + 2]-cycloaddition reaction which resulted in the synthesis of functionalized tricyclic ring systems containing an 8-oxabicyclo[3.2.1]octane core. Intramolecular ... ...

    Abstract We have the investigated base mediated asymmetric intramolecular oxidopyrylium-alkene [5 + 2]-cycloaddition reaction which resulted in the synthesis of functionalized tricyclic ring systems containing an 8-oxabicyclo[3.2.1]octane core. Intramolecular cycloaddition constructed two new rings, three new stereogenic centers, and provided a tricyclic cycloadduct with high diastereoselectivity and isolated yield. We incorporated an α-chiral center and an alkoxy alkene tether on the substrates and examined the effect of the size of alkyl groups and alkene tether length on diastereoselectivity. The requisite substrates for the oxidopyrylium-alkene cycloaddition reaction were synthesized in a few steps involving alkylation of optically active α-hydroxy amide, furyllithium addition, reduction of resulting ketone, and Achmatowicz reaction followed by acylation of a lactol intermediate. We have proposed stereochemical models for the [5 + 2] cycloaddition reaction via the oxidopyrylium ylide. Interestingly, the alkoxy substituent on the stereocenter and the chain length are responsible for the degree of stereoselectivity of the cycloadduct.
    MeSH term(s) Alkenes ; Cycloaddition Reaction ; Stereoisomerism
    Chemical Substances Alkenes
    Language English
    Publishing date 2021-05-20
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.1c00600
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article: Synthesis of amide derivatives for electron deficient amines and functionalized carboxylic acids using EDC and DMAP and a catalytic amount of HOBt as the coupling reagents

    Ghosh, Arun K / Shahabi, Dana

    Tetrahedron letters. 2021 Jan. 19, v. 63

    2021  

    Abstract: A convenient protocol for amide bond formation for electron deficient amines and carboxylic acids is described. Amide coupling of aniline derivatives has been investigated with a number of reagents under a variety of reaction conditions. The use of 1 ... ...

    Abstract A convenient protocol for amide bond formation for electron deficient amines and carboxylic acids is described. Amide coupling of aniline derivatives has been investigated with a number of reagents under a variety of reaction conditions. The use of 1 equivalent of EDC and 1 equivalent of DMAP, catalytic amount of HOBt and DIPEA provided the best results. This method is applicable for the synthesis of a range of functionalized amide derivatives with electron deficient and unreactive amines.
    Keywords aniline ; carboxylic acids ; protocols ; synthesis
    Language English
    Dates of publication 2021-0119
    Publishing place Elsevier Ltd
    Document type Article
    Note NAL-light
    ZDB-ID 204287-3
    ISSN 1873-3581 ; 0040-4039
    ISSN (online) 1873-3581
    ISSN 0040-4039
    DOI 10.1016/j.tetlet.2020.152719
    Database NAL-Catalogue (AGRICOLA)

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  10. Article ; Online: Lewis Acid-Catalyzed Vinyl Acetal Rearrangement of 4,5-Dihydro-1,3-dioxepines: Stereoselective Synthesis of

    Ghosh, Arun K / Belcher, Miranda R

    The Journal of organic chemistry

    2020  Volume 85, Issue 16, Page(s) 10399–10412

    Abstract: Lewis acid-catalyzed rearrangements of 4,5-dihydro-1,3-dioxepines have been investigated. Rearrangement of vinyl acetals under a variety of conditions resulted ... ...

    Abstract Lewis acid-catalyzed rearrangements of 4,5-dihydro-1,3-dioxepines have been investigated. Rearrangement of vinyl acetals under a variety of conditions resulted in
    MeSH term(s) Acetals ; Catalysis ; Furans ; Lewis Acids ; Stereoisomerism
    Chemical Substances Acetals ; Furans ; Lewis Acids
    Language English
    Publishing date 2020-08-05
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.0c00390
    Database MEDical Literature Analysis and Retrieval System OnLINE

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