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  1. Article: Studies on the preparation of aminobipyridines and bipyridine sultams via an intramolecular free radical pathway

    Recio, Javier / Filace, Fabiana / Gala, Elena / Pérez-Redondo, Adrián / Álvarez-Builla, Julio / Burgos, Carolina

    RSC advances. 2020 Mar. 11, v. 10, no. 18

    2020  

    Abstract: A variety of aminated bipyridines and bipyridine sultams are prepared by intramolecular radical [1,5]-ipso and [1,6]-ortho substitutions, using a sulfonamide as a linker to connect the pyridyl radical to the pyridine under attack. For the cases studied, ... ...

    Abstract A variety of aminated bipyridines and bipyridine sultams are prepared by intramolecular radical [1,5]-ipso and [1,6]-ortho substitutions, using a sulfonamide as a linker to connect the pyridyl radical to the pyridine under attack. For the cases studied, different regiochemistries are observed depending on the initial position of the sulfonamide linker.
    Keywords free radicals ; pyridines
    Language English
    Dates of publication 2020-0311
    Size p. 10447-10451.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ISSN 2046-2069
    DOI 10.1039/d0ra02026e
    Database NAL-Catalogue (AGRICOLA)

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  2. Article ; Online: Transcriptomic signature, bioactivity and safety of a non-hepatotoxic analgesic generating AM404 in the midbrain PAG region.

    Bazan, Hernan A / Bhattacharjee, Surjyadipta / Reid, Madigan M / Jun, Bokkyoo / Polk, Connor / Strain, Madeleine / St Pierre, Linsey A / Desai, Neehar / Daly, Patrick W / Cucinello-Ragland, Jessica A / Edwards, Scott / Recio, Javier / Alvarez-Builla, Julio / Cai, James J / Bazan, Nicolas G

    Scientific reports

    2024  Volume 14, Issue 1, Page(s) 11103

    Abstract: Safe and effective pain management is a critical healthcare and societal need. The potential for acute liver injury from paracetamol (ApAP) overdose; nephrotoxicity and gastrointestinal damage from chronic non-steroidal anti-inflammatory drug (NSAID) use; ...

    Abstract Safe and effective pain management is a critical healthcare and societal need. The potential for acute liver injury from paracetamol (ApAP) overdose; nephrotoxicity and gastrointestinal damage from chronic non-steroidal anti-inflammatory drug (NSAID) use; and opioids' addiction are unresolved challenges. We developed SRP-001, a non-opioid and non-hepatotoxic small molecule that, unlike ApAP, does not produce the hepatotoxic metabolite N-acetyl-p-benzoquinone-imine (NAPQI) and preserves hepatic tight junction integrity at high doses. CD-1 mice exposed to SRP-001 showed no mortality, unlike a 70% mortality observed with increasing equimolar doses of ApAP within 72 h. SRP-001 and ApAP have comparable antinociceptive effects, including the complete Freund's adjuvant-induced inflammatory von Frey model. Both induce analgesia via N-arachidonoylphenolamine (AM404) formation in the midbrain periaqueductal grey (PAG) nociception region, with SRP-001 generating higher amounts of AM404 than ApAP. Single-cell transcriptomics of PAG uncovered that SRP-001 and ApAP also share modulation of pain-related gene expression and cell signaling pathways/networks, including endocannabinoid signaling, genes pertaining to mechanical nociception, and fatty acid amide hydrolase (FAAH). Both regulate the expression of key genes encoding FAAH, 2-arachidonoylglycerol (2-AG), cannabinoid receptor 1 (CNR1), CNR2, transient receptor potential vanilloid type 4 (TRPV4), and voltage-gated Ca
    MeSH term(s) Animals ; Mice ; Transcriptome ; Acetaminophen/adverse effects ; Analgesics/pharmacology ; Arachidonic Acids/pharmacology ; Periaqueductal Gray/metabolism ; Periaqueductal Gray/drug effects ; Male ; Benzoquinones/pharmacology ; Glycerides ; Amidohydrolases/metabolism ; Amidohydrolases/genetics
    Language English
    Publishing date 2024-05-15
    Publishing country England
    Document type Journal Article
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-024-61791-z
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Studies on the preparation of aminobipyridines and bipyridine sultams

    Recio, Javier / Filace, Fabiana / Gala, Elena / Pérez-Redondo, Adrián / Álvarez-Builla, Julio / Burgos, Carolina

    RSC advances

    2020  Volume 10, Issue 18, Page(s) 10447–10451

    Abstract: A variety of aminated bipyridines and bipyridine sultams are prepared by intramolecular radical [1,5]- ...

    Abstract A variety of aminated bipyridines and bipyridine sultams are prepared by intramolecular radical [1,5]-
    Language English
    Publishing date 2020-03-11
    Publishing country England
    Document type Journal Article
    ISSN 2046-2069
    ISSN (online) 2046-2069
    DOI 10.1039/d0ra02026e
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: Transcriptomic signature, bioactivity and safety of a non-hepatoxic analgesic generating AM404 in the mid-brain PAG region.

    Bazan, Hernan / Bhattacharjee, Surjyadipta / Reid, Madigan / Jun, Bokkyoo / Polk, Connor / Strain, Madeleine / Pierre, Linsey St / Desai, Neehar / Daly, Patrick / Cucinello-Ragland, Jessica / Edwards, Scott / Alvarez-Builla, Julio / Cai, James / Bazan, Nicolas

    Research square

    2023  

    Abstract: The safe and effective management of pain is a critical healthcare and societal need. The potential for misuse and addiction associated with opioids, nephrotoxicity, and gastrointestinal damage from chronic non-steroidal anti-inflammatory drug (NSAID) ... ...

    Abstract The safe and effective management of pain is a critical healthcare and societal need. The potential for misuse and addiction associated with opioids, nephrotoxicity, and gastrointestinal damage from chronic non-steroidal anti-inflammatory drug (NSAID) use, as well as acute liver injury from paracetamol (ApAP) overdose, are unresolved challenges. To address them, we developed a non-opioid and non-hepatotoxic small molecule, SRP-001. Compared to ApAP, SRP-001 is not hepatotoxic as it does not produce N-acetyl-p-benzoquinone-imine (NAPQI) and maintains hepatic tight junction integrity at high doses. SRP-001 has comparable analgesia in pain models, including the complete Freund's adjuvant (CFA) inflammatory von Frey. Both induce analgesia via N-arachidonoylphenolamine (AM404) formation in the midbrain periaqueductal grey (PAG) nociception area, with SRP-001 generating higher amounts of AM404 than ApAP. Single-cell transcriptomics of PAG uncovered that SRP-001 and ApAP also share modulation of pain-related gene expression and cell signaling pathways, including the endocannabinoid, mechanical nociception, and fatty acid amide hydrolase (FAAH) pathways. Both regulate the expression of key genes encoding FAAH, 2-AG, CNR1, CNR2, TRPV4, and voltage-gated Ca2+ channel. Interim Phase 1 trial results demonstrate SRP-001's safety, tolerability, and favorable pharmacokinetics (NCT05484414). Given its non-hepatotoxicity and clinically validated analgesic mechanisms, SRP-001 offers a promising alternative to ApAP, NSAIDs, and opioids for safer pain treatment.
    Language English
    Publishing date 2023-05-04
    Publishing country United States
    Document type Preprint
    DOI 10.21203/rs.3.rs-2883310/v1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Effects of a Losartan-Antioxidant Hybrid (GGN1231) on Vascular and Cardiac Health in an Experimental Model of Chronic Renal Failure.

    Martínez-Arias, Laura / Fernández-Villabrille, Sara / Alonso-Montes, Cristina / García-Navazo, Gonzalo / Ruíz-Torres, María P / Alajarín, Ramón / Alvarez-Builla, Julio / Gutiérrez-Calabres, Elena / Vaquero-López, Juan José / Carrillo-López, Natalia / Rodríguez-Puyol, Diego / Cannata-Andía, Jorge B / Panizo, Sara / Naves-Díaz, Manuel

    Nutrients

    2023  Volume 15, Issue 8

    Abstract: Drugs providing antihypertensive and protective cardiovascular actions are of clinical interest in controlling cardiovascular events and slowing the progression of kidney disease. We studied the effect of a hybrid compound, GGN1231 (derived from losartan ...

    Abstract Drugs providing antihypertensive and protective cardiovascular actions are of clinical interest in controlling cardiovascular events and slowing the progression of kidney disease. We studied the effect of a hybrid compound, GGN1231 (derived from losartan in which a powerful antioxidant was attached), on the prevention of cardiovascular damage, cardiac hypertrophy, and fibrosis in a rat model of severe chronic renal failure (CRF). CRF by a 7/8 nephrectomy was carried out in male Wistar rats fed with a diet rich in phosphorous (0.9%) and normal calcium (0.6%) for a period of 12 weeks until sacrifice. In week 8, rats were randomized in five groups receiving different drugs including dihydrocaffeic acid as antioxidant (Aox), losartan (Los), dihydrocaffeic acid+losartan (Aox+Los) and GGN1231 as follows: Group 1 (CRF+vehicle group), Group 2 (CRF+Aox group), Group 3 (CRF+Los group), Group 4 (CRF+Aox+Los group), and Group 5 (CRF+GGN1231 group). Group 5, the CRF+GGN1231 group, displayed reduced proteinuria, aortic TNF-α, blood pressure, LV wall thickness, diameter of the cardiomyocytes, ATR1, cardiac TNF-α and fibrosis, cardiac collagen I, and TGF-β1 expression. A non-significant 20% reduction in the mortality was also observed. This study showed the possible advantages of GGN1231, which could help in the management of cardiovascular and inflammatory processes. Further research is needed to confirm and even expand the positive aspects of this compound.
    MeSH term(s) Rats ; Male ; Animals ; Losartan/pharmacology ; Losartan/therapeutic use ; Antioxidants/pharmacology ; Antioxidants/therapeutic use ; Tumor Necrosis Factor-alpha/pharmacology ; Rats, Wistar ; Kidney Failure, Chronic ; Models, Theoretical ; Fibrosis ; Kidney/metabolism
    Chemical Substances Losartan (JMS50MPO89) ; 3,4-dihydroxyphenylpropionic acid (1078-61-1) ; Antioxidants ; Tumor Necrosis Factor-alpha
    Language English
    Publishing date 2023-04-10
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2518386-2
    ISSN 2072-6643 ; 2072-6643
    ISSN (online) 2072-6643
    ISSN 2072-6643
    DOI 10.3390/nu15081820
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Book: Modern Heterocyclic Chemistry

    Alvarez-Builla, Julio / Barluenga, Jose

    2009  

    Author's details Hrsg. Jose Barluenga; Hrsg. Julio Alvarez-Builla
    Language English
    Size XX, 980 S. in 2 Bd., 1000 schw.-w. Ill., 5 farb. Ill, 240 mm x 170 mm
    Edition 1. Aufl.
    Publisher WILEY-VCH
    Publishing place Weinheim, Bergstr
    Document type Book
    ISBN 9783527312429 ; 3527312420
    Database Library catalogue of the German National Library of Science and Technology (TIB), Hannover

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  7. Article ; Online: Recent Advances in the Synthesis of Azonia Aromatic Heterocycles.

    Sucunza, David / Cuadro, Ana M / Alvarez-Builla, Julio / Vaquero, Juan J

    The Journal of organic chemistry

    2016  Volume 81, Issue 21, Page(s) 10126–10135

    Abstract: Azonia aromatic heterocycles are an important subclass of aza-heterocyles as they are the structural motif of relevant cationic alkaloids, and they have a wide range of potential applications such as bioactive compounds and organic materials. In this ... ...

    Abstract Azonia aromatic heterocycles are an important subclass of aza-heterocyles as they are the structural motif of relevant cationic alkaloids, and they have a wide range of potential applications such as bioactive compounds and organic materials. In this Synopsis, recent and novel approaches to their synthesis are surveyed, with particular emphasis on ring-closing metathesis reactions and annulation reactions based on C-H activation.
    Language English
    Publishing date 2016-11-04
    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.6b01092
    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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  8. Article: Recent Advances in the Synthesis of Azonia Aromatic Heterocycles

    Sucunza, David / Alvarez-Builla Julio / Cuadro Ana M / Vaquero Juan J

    Journal of organic chemistry. 2016 Nov. 04, v. 81, no. 21

    2016  

    Abstract: Azonia aromatic heterocycles are an important subclass of aza-heterocyles as they are the structural motif of relevant cationic alkaloids, and they have a wide range of potential applications such as bioactive compounds and organic materials. In this ... ...

    Abstract Azonia aromatic heterocycles are an important subclass of aza-heterocyles as they are the structural motif of relevant cationic alkaloids, and they have a wide range of potential applications such as bioactive compounds and organic materials. In this Synopsis, recent and novel approaches to their synthesis are surveyed, with particular emphasis on ring-closing metathesis reactions and annulation reactions based on C–H activation.
    Keywords alkaloids ; bioactive compounds ; carbon-hydrogen bond activation ; organic chemistry
    Language English
    Dates of publication 2016-1104
    Size p. 10126-10135.
    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.6b01092
    Database NAL-Catalogue (AGRICOLA)

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    In stock of ZB MED Bonn / Germany

    Z 4' 49/42: Show issues
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  9. Article ; Online: Prodrug approach: An overview of recent cases.

    Abet, Valentina / Filace, Fabiana / Recio, Javier / Alvarez-Builla, Julio / Burgos, Carolina

    European journal of medicinal chemistry

    2017  Volume 127, Page(s) 810–827

    Abstract: In this review we highlight the most modern trends in the prodrug strategy. In drug research and development, the prodrug concept has found a number of useful applications. Selected examples of this approach are provided in this paper and they are ... ...

    Abstract In this review we highlight the most modern trends in the prodrug strategy. In drug research and development, the prodrug concept has found a number of useful applications. Selected examples of this approach are provided in this paper and they are classified according to the aim of their design.
    MeSH term(s) Absorption, Physicochemical ; Animals ; Cell Membrane Permeability ; Drug Discovery/methods ; Humans ; Prodrugs/adverse effects ; Prodrugs/chemistry ; Prodrugs/metabolism ; Solubility ; Water/chemistry
    Chemical Substances Prodrugs ; Water (059QF0KO0R)
    Language English
    Publishing date 2017-02-15
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2016.10.061
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
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    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  10. Book: Modern heterocyclic chemistry

    Alvarez-Builla, Julio / Barluenga, José / Vaquero, Juan Jose

    2011  

    Author's details ed. by Julio Alvarez-Builla, Juan Jose Vaquero, and José Barluenga
    Language English
    Dates of publication 2011-9999
    Publisher Wiley-VCH
    Publishing place Weinheim
    Document type Book
    ISBN 3527332014 ; 9783527332014 ; 9783527634064 ; 3527634061
    Database Former special subject collection: coastal and deep sea fishing

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