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  1. Article ; Online: Insights into Newly Approved Drugs from a Medicinal Chemistry Perspective.

    Lima, Elys Juliane Cardoso / Gomes, Renan Augusto / Fornari, Evelin / da Silva Emery, Flavio / Trossini, Gustavo Henrique Goulart

    Mini reviews in medicinal chemistry

    2021  Volume 21, Issue 16, Page(s) 2227–2248

    Abstract: The development of new drugs is becoming notably harder each decade. To overcome the present pitfalls in the drug development pipeline, such as those related to potency, selectivity, or absorption, distribution, metabolism, excretion and toxicity ... ...

    Abstract The development of new drugs is becoming notably harder each decade. To overcome the present pitfalls in the drug development pipeline, such as those related to potency, selectivity, or absorption, distribution, metabolism, excretion and toxicity properties, medicinal chemistry strategies need to be in continuous evolution and need to become even more multidisciplinary. In this review, we present how structure-based, ligand-based, and fragment-based drug design (SBDD, LBDD, and FBDD, respectively) and their respective techniques were used for the design and optimization of successful cases of New Molecular Entities (NMEs) approved by the Food and Drug Administration (FDA).
    MeSH term(s) Chemistry, Pharmaceutical ; Drug Approval ; Drug Design ; Humans ; Ligands ; United States ; United States Food and Drug Administration/legislation & jurisprudence
    Chemical Substances Ligands
    Language English
    Publishing date 2021-02-26
    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 10.2174/1389557521666210226145328
    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:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  2. Article ; Online: Parasitic sirtuin 2 as an opportunity in drug discovery.

    Gomes, Renan Augusto / Fornari, Evelin / Silva Rocha, Ana Carolina / Tripodi, Gustavo Luis / Silva Emery, Flavio da / Goulart Trossini, Gustavo Henrique

    Future medicinal chemistry

    2021  Volume 13, Issue 16, Page(s) 1397–1409

    Abstract: Infections caused by protozoans remain a public health issue, especially in tropical countries. Serious adverse events, lack of efficacy at the different stages of the infection and routes of administration that have a negative impact on treatment ... ...

    Abstract Infections caused by protozoans remain a public health issue, especially in tropical countries. Serious adverse events, lack of efficacy at the different stages of the infection and routes of administration that have a negative impact on treatment adherence are some of the problems with currently available therapy against these diseases. Here we describe an epigenetic target, sirtuin 2 and its related proteins, that is promising given the results in phenotypic assays and
    MeSH term(s) Animals ; Antiprotozoal Agents/chemistry ; Antiprotozoal Agents/pharmacology ; Drug Discovery ; Humans ; Leishmania/drug effects ; Parasitic Sensitivity Tests ; Plasmodium falciparum/drug effects ; Schistosoma mansoni/drug effects ; Sirtuin 2/antagonists & inhibitors ; Sirtuin 2/metabolism ; Trypanosoma/drug effects
    Chemical Substances Antiprotozoal Agents ; Sirtuin 2 (EC 3.5.1.-)
    Language English
    Publishing date 2021-06-30
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2021-0091
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Synthesis of α-amino-1,3-dicarbonyl compounds via Ugi flow chemistry reaction: access to functionalized 1,2,3-triazoles.

    Vasconcelos, Stanley N S / Fornari, Evelin / Caracelli, Ignez / Stefani, Hélio A

    Molecular diversity

    2017  Volume 21, Issue 4, Page(s) 893–902

    Abstract: The Ugi multicomponent reaction has been used as an important synthetic route to obtain compounds with potential biological activity. We present the rapid and efficient synthesis of [Formula: see text]-amino-1,3-dicarbonyl compounds in moderate to good ... ...

    Abstract The Ugi multicomponent reaction has been used as an important synthetic route to obtain compounds with potential biological activity. We present the rapid and efficient synthesis of [Formula: see text]-amino-1,3-dicarbonyl compounds in moderate to good yields via Ugi flow chemistry reactions performed with a continuous flow reactor. Such [Formula: see text]-amino-1,3-dicarbonyl compounds can act as precursors for the production of [Formula: see text]-amino acids via hydrolysis of the ethyl ester group as well as building blocks for the synthesis of novel compounds with the 1,2,3-triazole ring. The [Formula: see text]-amino acid derivatives of the Ugi flow chemistry reaction products were then used for dipeptide synthesis.
    MeSH term(s) Aldehydes/chemistry ; Chemistry Techniques, Synthetic ; Click Chemistry ; Models, Molecular ; Molecular Conformation ; Stereoisomerism ; Triazoles/chemical synthesis ; Triazoles/chemistry
    Chemical Substances Aldehydes ; Triazoles
    Language English
    Publishing date 2017-07-12
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1376507-3
    ISSN 1573-501X ; 1381-1991
    ISSN (online) 1573-501X
    ISSN 1381-1991
    DOI 10.1007/s11030-017-9764-5
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4946: Show issues Location:
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    ab Jg. 2022: Lesesaal (EG)

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