LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 274

Search options

  1. Article ; Online: BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α

    Meibom, Daniel / Meyer, Jutta / von Buehler, Clemens-Jeremias / Collins, Karl D / Maassen, Stefanie / Gericke, Kersten Matthias / Hüser, Jörg / Mittendorf, Joachim / Ortega Hernandez, Nuria / Schamberger, Jens / Stampfuss, Jan / Straub, Alexander / Torge, Afra / Witowski, Norbert / Wunder, Frank

    Journal of medicinal chemistry

    2023  Volume 66, Issue 7, Page(s) 4659–4670

    Abstract: After acute myocardial infarction, early reperfusion is the most effective strategy for reducing cardiac damage and improving clinical outcome. However, restoring blood flow to the ischemic myocardium can paradoxically induce injury by itself ( ... ...

    Abstract After acute myocardial infarction, early reperfusion is the most effective strategy for reducing cardiac damage and improving clinical outcome. However, restoring blood flow to the ischemic myocardium can paradoxically induce injury by itself (reperfusion injury), with microvascular dysfunction being one contributing factor. α
    MeSH term(s) Rats ; Animals ; Adrenergic Agents
    Chemical Substances Adrenergic Agents
    Language English
    Publishing date 2023-03-18
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c01690
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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: BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor.

    Meibom, Daniel / Wasnaire, Pierre / Beyer, Kristin / Broehl, Andreas / Cancho-Grande, Yolanda / Elowe, Nadine / Henninger, Kerstin / Johannes, Sarah / Jungmann, Natalia / Krainz, Tanja / Lindner, Niels / Maassen, Stefanie / MacDonald, Bryan / Menshykau, Denis / Mittendorf, Joachim / Sanchez, Guzman / Schaefer, Martina / Stefan, Eric / Torge, Afra /
    Xing, Yi / Zubov, Dmitry

    Journal of medicinal chemistry

    2024  Volume 67, Issue 4, Page(s) 2907–2940

    Abstract: The matrix metalloprotease ADAMTS7 has been identified by multiple genome-wide association studies as being involved in the development of coronary artery disease. Subsequent research revealed the proteolytic function of the enzyme to be relevant for ... ...

    Abstract The matrix metalloprotease ADAMTS7 has been identified by multiple genome-wide association studies as being involved in the development of coronary artery disease. Subsequent research revealed the proteolytic function of the enzyme to be relevant for atherogenesis and restenosis after vessel injury. Based on a publicly known dual ADAMTS4/ADAMTS5 inhibitor, we have in silico designed an ADAMTS7 inhibitor of the catalytic domain, which served as a starting point for an optimization campaign. Initially our inhibitors suffered from low selectivity vs MMP12. An X-ray cocrystal structure inspired us to exploit amino acid differences in the binding site of MMP12 and ADAMTS7 to improve selectivity. Further optimization composed of employing 5-membered heteroaromatic groups as hydantoin substituents to become more potent on ADAMTS7. Finally, fine-tuning of DMPK properties yielded BAY-9835, the first orally bioavailable ADAMTS7 inhibitor. Further optimization to improve selectivity vs ADAMTS12 seems possible, and a respective starting point could be identified.
    MeSH term(s) Humans ; ADAMTS7 Protein/genetics ; ADAMTS7 Protein/metabolism ; Genome-Wide Association Study ; Matrix Metalloproteinase 12 ; Atherosclerosis ; Coronary Artery Disease
    Chemical Substances ADAMTS7 Protein (EC 3.4.24.-) ; Matrix Metalloproteinase 12 (EC 3.4.24.65) ; ADAMTS7 protein, human (EC 3.4.24.-)
    Language English
    Publishing date 2024-02-13
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c02036
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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.

  3. Book: Vergleich der Schlachtvieh- und Fleischpreise in der Großhandelsstufe in den Ländern der EWG

    Mittendorf, Hans-Joachim

    1961  

    Title variant Schlachtviehpreise
    Author's details Hans-Joachim Mittendorf
    Language German
    Size 86 Bl. : Ill., graph. Darst., Kt.
    Publisher Inst. f. Landw. Marktforschung
    Publishing place Braunschweig-Völkenrode
    Publishing country Germany
    Document type Book
    Note Maschinenschr. vervielf.
    HBZ-ID HT009733870
    Database Catalogue ZB MED Nutrition, Environment, Agriculture

    More links

    Kategorien

    In stock of ZB MED Bonn / Germany

    Shelf markLoan statusLocation
    824/418 order for loan Geschlossenes Magazin (U2)

    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.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  4. Article ; Online: New Generation of sGC Stimulators: Discovery of Imidazo[1,2-

    Vakalopoulos, Alexandros / Wunder, Frank / Hartung, Ingo V / Redlich, Gorden / Jautelat, Rolf / Buchgraber, Philipp / Hassfeld, Jorma / Gromov, Alexey V / Lindner, Niels / Bierer, Donald / Gries, Jörg / Kroh, Walter / Paulsen, Holger / Mittendorf, Joachim / Lang, Dieter / Becker-Pelster, Eva / Brockschnieder, Damian / Geiss, Volker / Li, Volkhart /
    Straub, Alexander / Knorr, Andreas / Mondritzki, Thomas / Trübel, Hubert / Raschke, Marian / Schaefer, Martina / Thomas, Dirk / Sandner, Peter / Stasch, Johannes-Peter / Follmann, Markus

    Journal of medicinal chemistry

    2023  Volume 66, Issue 11, Page(s) 7280–7303

    Abstract: Herein, we describe the identification, chemical optimization, and preclinical characterization of novel soluble guanylate cyclase (sGC) stimulators. Given the very broad therapeutic opportunities for sGC stimulators, new tailored molecules for distinct ... ...

    Abstract Herein, we describe the identification, chemical optimization, and preclinical characterization of novel soluble guanylate cyclase (sGC) stimulators. Given the very broad therapeutic opportunities for sGC stimulators, new tailored molecules for distinct indications with specific pharmacokinetics, tissue distribution, and physicochemical properties will be required in the future. Here, we report the ultrahigh-throughput (uHTS)-based discovery of a new class of sGC stimulators from an imidazo[1,2-
    MeSH term(s) Humans ; Soluble Guanylyl Cyclase/metabolism ; Guanylate Cyclase/metabolism ; Hypertension/drug therapy ; Vasodilator Agents ; Pyridines/pharmacology ; Pyridines/therapeutic use ; Nitric Oxide/metabolism
    Chemical Substances Soluble Guanylyl Cyclase (EC 4.6.1.2) ; Guanylate Cyclase (EC 4.6.1.2) ; 2-(2-Chloro-4-(methylsulfonyl)-3-((2,2,2-trifluoroethoxy)methyl)benzoyl)-1,3-cyclohexanedione (BAY 747) ; Vasodilator Agents ; Pyridines ; Nitric Oxide (31C4KY9ESH)
    Language English
    Publishing date 2023-04-11
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c02082
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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.

  5. Article ; Online: Structure-Permeability Relationship of Semipeptidic Macrocycles-Understanding and Optimizing Passive Permeability and Efflux Ratio.

    Le Roux, Antoine / Blaise, Émilie / Boudreault, Pierre-Luc / Comeau, Christian / Doucet, Annie / Giarrusso, Marilena / Collin, Marie-Pierre / Neubauer, Thomas / Kölling, Florian / Göller, Andreas H / Seep, Lea / Tshitenge, Dieudonné T / Wittwer, Matthias / Kullmann, Maximilian / Hillisch, Alexander / Mittendorf, Joachim / Marsault, Eric

    Journal of medicinal chemistry

    2020  Volume 63, Issue 13, Page(s) 6774–6783

    Abstract: We herein report the first thorough analysis of the structure-permeability relationship of semipeptidic macrocycles. In total, 47 macrocycles were synthesized using a hybrid solid-phase/solution strategy, and then their passive and cellular permeability ... ...

    Abstract We herein report the first thorough analysis of the structure-permeability relationship of semipeptidic macrocycles. In total, 47 macrocycles were synthesized using a hybrid solid-phase/solution strategy, and then their passive and cellular permeability was assessed using the parallel artificial membrane permeability assay (PAMPA) and Caco-2 assay, respectively. The results indicate that semipeptidic macrocycles generally possess high passive permeability based on the PAMPA, yet their cellular permeability is governed by efflux, as reported in the Caco-2 assay. Structural variations led to tractable structure-permeability and structure-efflux relationships, wherein the linker length, stereoinversion, N-methylation, and peptoids site-specifically impact the permeability and efflux. Extensive nuclear magnetic resonance, molecular dynamics, and ensemble-based three-dimensional polar surface area (3D-PSA) studies showed that ensemble-based 3D-PSA is a good predictor of passive permeability.
    MeSH term(s) Caco-2 Cells ; Humans ; Macrocyclic Compounds/chemistry ; Macrocyclic Compounds/metabolism ; Membranes, Artificial ; Peptides/chemistry ; Permeability
    Chemical Substances Macrocyclic Compounds ; Membranes, Artificial ; Peptides
    Language English
    Publishing date 2020-05-26
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c00013
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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.

  6. Book: Livestock and meat marketing in Africa

    Mittendorf, Hans-Joachim / Wilson, S. G.

    report of a survey

    1961  

    Institution African Livestock and Meat Marketing Centre
    Author's details by H.J. Mittendorf and S.G. Wilson, special FAO consultants and the Centre at Fort Lamy, Chad, 5-22 December 1960
    Language English
    Size 123 Seiten, Diagramme, Karten
    Publisher Food and Agriculture Organization of the United Nations
    Publishing place Rome
    Publishing country Italy
    Document type Book
    HBZ-ID HT021120907
    Database Catalogue ZB MED Nutrition, Environment, Agriculture

    More links

    Kategorien

    In stock of ZB MED Bonn / Germany

    Shelf markLoan statusLocation
    844/523 order for loan Geschlossenes Magazin (U2)
    Fotokopie

    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.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  7. Article ; Online: Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A

    Meibom, Daniel / Albrecht-Küpper, Barbara / Diedrichs, Nicole / Hübsch, Walter / Kast, Raimund / Krämer, Thomas / Krenz, Ursula / Lerchen, Hans-Georg / Mittendorf, Joachim / Nell, Peter G / Süssmeier, Frank / Vakalopoulos, Alexandros / Zimmermann, Katja

    ChemMedChem

    2017  Volume 12, Issue 10, Page(s) 728–737

    Abstract: Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine ... ...

    Abstract Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A
    MeSH term(s) Adenosine A1 Receptor Agonists/administration & dosage ; Adenosine A1 Receptor Agonists/chemistry ; Adenosine A1 Receptor Agonists/pharmacology ; Administration, Oral ; Animals ; Chronic Disease ; Dipeptides/administration & dosage ; Dipeptides/chemistry ; Dipeptides/pharmacology ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Heart Diseases/drug therapy ; Humans ; Injections, Intravenous ; Molecular Structure ; Prodrugs/administration & dosage ; Prodrugs/chemistry ; Prodrugs/pharmacology ; Pyridines/administration & dosage ; Pyridines/chemistry ; Pyridines/pharmacology ; Rats ; Receptor, Adenosine A1/metabolism ; Solubility ; Structure-Activity Relationship
    Chemical Substances Adenosine A1 Receptor Agonists ; Dipeptides ; Prodrugs ; Pyridines ; Receptor, Adenosine A1 ; neladenoson bialanate
    Language English
    Publishing date 2017-05-22
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.201700151
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 6280: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    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.

  8. Article ; Online: Discovery of the Soluble Guanylate Cyclase Activator Runcaciguat (BAY 1101042).

    Hahn, Michael G / Lampe, Thomas / El Sheikh, Sherif / Griebenow, Nils / Woltering, Elisabeth / Schlemmer, Karl-Heinz / Dietz, Lisa / Gerisch, Michael / Wunder, Frank / Becker-Pelster, Eva-Maria / Mondritzki, Thomas / Tinel, Hanna / Knorr, Andreas / Kern, Armin / Lang, Dieter / Hueser, Joerg / Schomber, Tibor / Benardeau, Agnes / Eitner, Frank /
    Truebel, Hubert / Mittendorf, Joachim / Kumar, Vijay / van den Akker, Focco / Schaefer, Martina / Geiss, Volker / Sandner, Peter / Stasch, Johannes-Peter

    Journal of medicinal chemistry

    2021  Volume 64, Issue 9, Page(s) 5323–5344

    Abstract: Herein we describe the discovery, mode of action, and preclinical characterization of the soluble guanylate cyclase (sGC) activator runcaciguat. The sGC enzyme, via the formation of cyclic guanosine monophoshphate, is a key regulator of body and tissue ... ...

    Abstract Herein we describe the discovery, mode of action, and preclinical characterization of the soluble guanylate cyclase (sGC) activator runcaciguat. The sGC enzyme, via the formation of cyclic guanosine monophoshphate, is a key regulator of body and tissue homeostasis. sGC activators with their unique mode of action are activating the oxidized and heme-free and therefore NO-unresponsive form of sGC, which is formed under oxidative stress. The first generation of sGC activators like cinaciguat or ataciguat exhibited limitations and were discontinued. We overcame limitations of first-generation sGC activators and identified a new chemical class via high-throughput screening. The investigation of the structure-activity relationship allowed to improve potency and multiple solubility, permeability, metabolism, and drug-drug interactions parameters. This program resulted in the discovery of the oral sGC activator runcaciguat (compound
    MeSH term(s) Animals ; Binding Sites ; Crystallography, X-Ray ; Cytochrome P-450 CYP3A/chemistry ; Cytochrome P-450 CYP3A/metabolism ; Dogs ; Drug Design ; Enzyme Activators/chemistry ; Enzyme Activators/metabolism ; Enzyme Activators/pharmacology ; Enzyme Activators/therapeutic use ; Half-Life ; Heart Rate/drug effects ; Hemodynamics/drug effects ; Hypertension/drug therapy ; Hypertension/pathology ; Molecular Dynamics Simulation ; Rats ; Rats, Inbred SHR ; Solubility ; Soluble Guanylyl Cyclase/chemistry ; Soluble Guanylyl Cyclase/metabolism ; Structure-Activity Relationship
    Chemical Substances Enzyme Activators ; Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Soluble Guanylyl Cyclase (EC 4.6.1.2)
    Language English
    Publishing date 2021-04-19
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c02154
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

    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.

  9. Article ; Online: Identification of acidic heterocycle-substituted 1H-pyrazolo[3,4-b]pyridines as soluble guanylate cyclase stimulators.

    Griebenow, Nils / Schirok, Hartmut / Mittendorf, Joachim / Straub, Alexander / Follmann, Markus / Stasch, Johannes-Peter / Knorr, Andreas / Schlemmer, Karl-Heinz / Redlich, Gorden

    Bioorganic & medicinal chemistry letters

    2013  Volume 23, Issue 5, Page(s) 1197–1200

    Abstract: Novel guanylate cyclase stimulators are disclosed. Design, synthesis, SAR, and pharmacological profile of the compounds are discussed. ...

    Abstract Novel guanylate cyclase stimulators are disclosed. Design, synthesis, SAR, and pharmacological profile of the compounds are discussed.
    MeSH term(s) Animals ; Guanylate Cyclase/chemistry ; Guanylate Cyclase/metabolism ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Pyridines/pharmacology ; Rats ; Stimulation, Chemical ; Structure-Activity Relationship
    Chemical Substances Pyrazoles ; Pyridines ; Guanylate Cyclase (EC 4.6.1.2)
    Language English
    Publishing date 2013-03-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2013.01.028
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: 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.

  10. Book ; Thesis: Über eine neuartige Ringerweiterung von 1,4-Dihydropyrazinen zu 1,4-Diazepinen und von Benzodihydroaromaten zu Benzocycloheptatrienyl-Derivaten

    Mittendorf, Joachim

    1989  

    Author's details von Joachim Mittendorf
    Language German
    Size 196 S, graph. Darst
    Document type Book ; Thesis
    Thesis / German Habilitation thesis Univ., Diss.--Göttingen, 1989
    Database Former special subject collection: coastal and deep sea fishing

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

To top