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  1. Article ; Online: A Mini Review on Emerging Targets and Approaches for the Synthesis of Anti-viral Compounds: In Perspective to COVID-19.

    Gokada, Maheswara Rao / Pasupuleti, Visweswara Rao / Bollikolla, Hari Babu

    Mini reviews in medicinal chemistry

    2021  Volume 21, Issue 10, Page(s) 1173–1181

    Abstract: The novel Coronavirus disease (COVID-19) is an epidemic disease that appeared at the end of the year 2019 with a sudden increase in number and came to be considered as a pandemic disease caused by a viral infection which has threatened most countries for ...

    Abstract The novel Coronavirus disease (COVID-19) is an epidemic disease that appeared at the end of the year 2019 with a sudden increase in number and came to be considered as a pandemic disease caused by a viral infection which has threatened most countries for an emergency search for new anti-SARS-COV drugs /vaccines. At present, the number of clinical trials is ongoing worldwide on different drugs i.e. Hydroxychloroquine, Remedisvir, Favipiravir that utilize various mechanisms of action. A few countries are currently processing clinical trials, which may result in a positive outcome. Favipiravir (FPV) represents one of the feasible treatment options for COVID-19, if the result of the trials turns out positive. Favipiravir will be one of the developed possibly authoritative drugs to warrant benefits to mankind with large-scale production to meet the demands of the current pandemic Covid-19 outbreak and future epidemic outbreaks. In this review, the authors tried to explore key molecules, which will be supportive for devising COVID-19 research.
    MeSH term(s) Antiviral Agents/chemical synthesis ; Antiviral Agents/therapeutic use ; COVID-19/drug therapy ; COVID-19/virology ; Drug Delivery Systems ; Humans ; SARS-CoV-2/drug effects
    Chemical Substances Antiviral Agents
    Language English
    Publishing date 2021-01-04
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 2104081-3
    ISSN 1875-5607 ; 1389-5575
    ISSN (online) 1875-5607
    ISSN 1389-5575
    DOI 10.2174/1389557521666210104165733
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5891: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
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  2. Article ; Online: Catalytic enantioselective acyl transfer: the case for 4-PPY with a C-3 carboxamide peptide auxiliary based on synthesis and modelling studies.

    Cozett, Rudy E / Venter, Gerhard A / Gokada, Maheswara Rao / Hunter, Roger

    Organic & biomolecular chemistry

    2016  Volume 14, Issue 46, Page(s) 10914–10925

    Abstract: A series of 4-pyrrolidinopyridine (4-PPY) C-3 carboxamides containing peptide-based side chains have been synthesised and evaluated in the kinetic resolution of a small library of chiral benzylic secondary alcohols. A key design element was the ... ...

    Abstract A series of 4-pyrrolidinopyridine (4-PPY) C-3 carboxamides containing peptide-based side chains have been synthesised and evaluated in the kinetic resolution of a small library of chiral benzylic secondary alcohols. A key design element was the incorporation of a tryptophan residue in the peptide side chain for promoting π-stacking between peptide side chain and the pyridinium ring of the N-acyl intermediate, in which modelling was used as a structure-based guiding tool. Together, a catalyst containing a LeuTrp-N-Boc side chain (catalyst 8) was identified that achieved s-values up to and in slight excess of 10. A transition-state model based on the modelling is proposed to explain the origin of enantioselectivity. This study establishes the usefulness of modelling as a structure-based guiding tool for enantioselectivity optimization as well as the potential for developing scalable peptide-based DMAP-type catalysts for large-scale resolution work.
    Language English
    Publishing date 2016-11-22
    Publishing country England
    Document type Journal Article
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/c6ob01991a
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Quaternized α,α′-Amino Acids via Curtius Rearrangement of Substituted Malonate–Imidazolidinones

    Gokada, Maheswara Rao / Andrijevic Ana / Hunter Roger / Petersen Wade F / Rees-Jones Sophie / Samanta Sauvik / Venter Gerhard

    Journal of organic chemistry. 2017 Oct. 06, v. 82, no. 19

    2017  

    Abstract: An efficient synthesis protocol is presented for accessing quaternized α-amino acids in chiral, nonracemic form via diastereoselective malonate alkylation followed by C- to N-transposition. The key stereodifferentiating step involves a ... ...

    Abstract An efficient synthesis protocol is presented for accessing quaternized α-amino acids in chiral, nonracemic form via diastereoselective malonate alkylation followed by C- to N-transposition. The key stereodifferentiating step involves a diastereoselective alkylation of an α-monosubstituted malonate–imidazolidinone, which is followed first by a chemoselective malonate PMB ester removal and then a Curtius rearrangement to provide the transposition. The method demonstrates a high product ee (89–99% for eight cases) for quaternizing a range of proteinogenic α-amino acids. The stereogenicity in targets 5a–i supports previous conclusions that the diastereoselective alkylation step proceeds via an α-substituted malonate–imidazolidinone enolate in its Z-configuration, with the auxiliary in an s-transC–N conformation.
    Keywords acids ; alkylation ; amino acids ; chemical structure ; chemoselectivity ; diastereoselectivity ; organic chemistry ; organic compounds
    Language English
    Dates of publication 2017-1006
    Size p. 10650-10658.
    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%2Facs.joc.7b01684
    Database NAL-Catalogue (AGRICOLA)

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  4. Article ; Online: Quaternized α,α'-Amino Acids via Curtius Rearrangement of Substituted Malonate-Imidazolidinones.

    Gokada, Maheswara Rao / Hunter, Roger / Andrijevic, Ana / Petersen, Wade F / Samanta, Sauvik / Venter, Gerhard / Rees-Jones, Sophie

    The Journal of organic chemistry

    2017  Volume 82, Issue 19, Page(s) 10650–10658

    Abstract: An efficient synthesis protocol is presented for accessing quaternized α-amino acids in chiral, nonracemic form via diastereoselective malonate alkylation followed by C- to N-transposition. The key stereodifferentiating step involves a diastereoselective ...

    Abstract An efficient synthesis protocol is presented for accessing quaternized α-amino acids in chiral, nonracemic form via diastereoselective malonate alkylation followed by C- to N-transposition. The key stereodifferentiating step involves a diastereoselective alkylation of an α-monosubstituted malonate-imidazolidinone, which is followed first by a chemoselective malonate PMB ester removal and then a Curtius rearrangement to provide the transposition. The method demonstrates a high product ee (89-99% for eight cases) for quaternizing a range of proteinogenic α-amino acids. The stereogenicity in targets 5a-i supports previous conclusions that the diastereoselective alkylation step proceeds via an α-substituted malonate-imidazolidinone enolate in its Z-configuration, with the auxiliary in an s-trans
    Language English
    Publishing date 2017-10-06
    Publishing country United States
    Document type Journal Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.7b01684
    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:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
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    ab Jg. 2022: Lesesaal (EG)

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