LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 2 of total 2

Search options

  1. Article ; Online: Synthesis, Docking Study and Biological Evaluation of Amide-Based Soluble Epoxide Hydrolase Inhibitors with Novel Secondary Pharmacophore of Pyrimidin-2-ol.

    Hejazi, Leila / Ebadi, Abraham / Fakhar, Zeynab / Nazari, Maryam / Rezaee, Elham / Abbas Tabatabai, Sayyed

    Chemistry & biodiversity

    2022  Volume 19, Issue 11, Page(s) e202200231

    Abstract: Soluble epoxide hydrolase enzyme (sEH) is one of the most promising and emerging targets to develop drugs for multiple disease indications, including hypertension, diabetes, stroke, dyslipidemia, pain, etc. Most inhibitor scaffolds have a urea or amide ... ...

    Abstract Soluble epoxide hydrolase enzyme (sEH) is one of the most promising and emerging targets to develop drugs for multiple disease indications, including hypertension, diabetes, stroke, dyslipidemia, pain, etc. Most inhibitor scaffolds have a urea or amide moiety to mimic the active-site transition state. In this regard, we developed a series of amide sEH inhibitors with a pyrimidin-2-ol ring as a new secondary pharmacophore, which was subjected to in vitro evaluation. Compound 4w (4-chloro-N-{4-[6-(4-chlorophenyl)-2-hydroxypyrimidin-4-yl]phenyl}benzamide), which contains 4-chloro substituent in both terminal phenyl rings, exhibited the most inhibitory activity against sEH with an IC
    MeSH term(s) Epoxide Hydrolases/chemistry ; Epoxide Hydrolases/metabolism ; Amides/pharmacology ; Amides/chemistry ; Molecular Docking Simulation ; Structure-Activity Relationship ; Urea/pharmacology ; Urea/chemistry ; Enzyme Inhibitors/chemistry ; Solubility
    Chemical Substances Epoxide Hydrolases (EC 3.3.2.-) ; Amides ; Urea (8W8T17847W) ; Enzyme Inhibitors
    Language English
    Publishing date 2022-10-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2139001-0
    ISSN 1612-1880 ; 1612-1872
    ISSN (online) 1612-1880
    ISSN 1612-1872
    DOI 10.1002/cbdv.202200231
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  2. Article ; Online: 5-[Aryloxypyridyl (or nitrophenyl)]-4H-1,2,4-triazoles as novel flexible benzodiazepine analogues: Synthesis, receptor binding affinity and lipophilicity-dependent anti-seizure onset of action.

    Navidpour, Latifeh / Shabani, Shabnam / Heidari, Alireza / Bashiri, Manouchehr / Ebrahim-Habibi, Azadeh / Shahhosseini, Soraya / Shafaroodi, Hamed / Abbas Tabatabai, Sayyed / Toolabi, Mahsa

    Bioorganic chemistry

    2020  Volume 106, Page(s) 104504

    Abstract: A new series of 5-(2-aryloxy-4-nitrophenyl)-4H-1,2,4-triazoles and 5-(2-aryloxy-3-pyridyl)-4H-1,2,4-triazoles, possessing C-3 thio or alkylthio substituents, was synthesized and evaluated for their benzodiazepine receptor affinity and anti-seizure ... ...

    Abstract A new series of 5-(2-aryloxy-4-nitrophenyl)-4H-1,2,4-triazoles and 5-(2-aryloxy-3-pyridyl)-4H-1,2,4-triazoles, possessing C-3 thio or alkylthio substituents, was synthesized and evaluated for their benzodiazepine receptor affinity and anti-seizure activity. These analogues revealed similar to significantly superior affinity to GABA
    MeSH term(s) Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/chemistry ; Anticonvulsants/pharmacology ; Benzodiazepines/chemical synthesis ; Benzodiazepines/chemistry ; Benzodiazepines/pharmacology ; Binding, Competitive/drug effects ; Dose-Response Relationship, Drug ; Hydrophobic and Hydrophilic Interactions ; Male ; Molecular Structure ; Rats ; Rats, Sprague-Dawley ; Receptors, GABA-A/chemistry ; Seizures/drug therapy ; Structure-Activity Relationship ; Triazoles/chemical synthesis ; Triazoles/chemistry ; Triazoles/pharmacology
    Chemical Substances Anticonvulsants ; Receptors, GABA-A ; Triazoles ; Benzodiazepines (12794-10-4) ; 1,2,4-triazole (288-88-0)
    Language English
    Publishing date 2020-11-24
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.104504
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: 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)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top