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  1. Article ; Online: New β-glucan inhibitors as antifungal drugs.

    Hector, Richard F / Bierer, Donald E

    Expert opinion on therapeutic patents

    2011  Volume 21, Issue 10, Page(s) 1597–1610

    Abstract: Introduction: New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the ... ...

    Abstract Introduction: New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, micafungin and anidulafungin.
    Area covered: This review covers applications disclosing compound classes that include synthetic pyridazinone analogs, bicyclic heteroaryl ring compounds, aniline derivates, and semi-synthetic echinocandin and enfumafungin derivatives. MK-3118 is an analog of the natural product enfumafungin that, in particular, shows promise as it has a spectrum of activity comparable with caspofungin but has the advantageous property of oral bioavailability.
    Expert opinion: The diversity of chemical classes in the present review, which have demonstrable activity against β-glucan and the prospect of oral bioavailability, offers hope that safe and effective antifungal drugs will emerge and be commercialized. Of particular note, the Merck compound MK-3118, with solid evidence of efficacy based on preclinical data, has moved into clinical trials.
    MeSH term(s) Administration, Oral ; Animals ; Antifungal Agents/adverse effects ; Antifungal Agents/pharmacokinetics ; Antifungal Agents/pharmacology ; Biological Availability ; Drug Design ; Glycosides/pharmacokinetics ; Glycosides/pharmacology ; Humans ; Mycoses/drug therapy ; Mycoses/microbiology ; Patents as Topic ; Triterpenes/pharmacokinetics ; Triterpenes/pharmacology ; beta-Glucans/antagonists & inhibitors
    Chemical Substances Antifungal Agents ; Glycosides ; Triterpenes ; beta-Glucans ; ibrexafungerp (A92JFM5XNU)
    Language English
    Publishing date 2011-07-25
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1186201-4
    ISSN 1744-7674 ; 0962-2594 ; 1354-3776
    ISSN (online) 1744-7674
    ISSN 0962-2594 ; 1354-3776
    DOI 10.1517/13543776.2011.603899
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3962: Show issues Location:
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  2. Article ; Online: Total Synthesis of Cacalol.

    Garofalo, Albert W. / Litvak, Joane / Wang, Lisa / Dubenko, Larisa G. / Cooper, Raymond / Bierer, Donald E.

    The Journal of organic chemistry

    1999  Volume 64, Issue 9, Page(s) 3369–3372

    Language English
    Publishing date 1999-04-30
    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/jo9822838
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 4473: Show issues Location:
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  3. Article: Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.

    Rudolph, Joachim / Esler, William P / O'connor, Stephen / Coish, Philip D G / Wickens, Philip L / Brands, Michael / Bierer, Donald E / Bloomquist, Brian T / Bondar, Georgiy / Chen, Libing / Chuang, Chih-Yuan / Claus, Thomas H / Fathi, Zahra / Fu, Wenlang / Khire, Uday R / Kristie, James A / Liu, Xiao-Gao / Lowe, Derek B / McClure, Andrea C /
    Michels, Martin / Ortiz, Astrid A / Ramsden, Philip D / Schoenleber, Robert W / Shelekhin, Tatiana E / Vakalopoulos, Alexandros / Tang, Weifeng / Wang, Lei / Yi, Lin / Gardell, Stephen J / Livingston, James N / Sweet, Laurel J / Bullock, William H

    Journal of medicinal chemistry

    2007  Volume 50, Issue 21, Page(s) 5202–5216

    Abstract: The peptide hormone ghrelin is the endogenous ligand for the type 1a growth hormone secretagogue receptor (GHS-R1a) and the only currently known circulating appetite stimulant. GHS-R1a antagonism has therefore been proposed as a potential approach for ... ...

    Abstract The peptide hormone ghrelin is the endogenous ligand for the type 1a growth hormone secretagogue receptor (GHS-R1a) and the only currently known circulating appetite stimulant. GHS-R1a antagonism has therefore been proposed as a potential approach for obesity treatment. More recently, ghrelin has been recognized to also play a role in controlling glucose-induced insulin secretion, which suggests another possible benefit for a GHS-R1a antagonist, namely, the role as an insulin secretagogue with potential value for diabetes treatment. In our laboratories, piperidine-substituted quinazolinone derivatives were identified as a new class of small-molecule GHS-R1a antagonists. Starting from an agonist with poor oral bioavailability, optimization led to potent, selective, and orally bioavailable antagonists. In vivo efficacy evaluation of selected compounds revealed suppression of food intake and body weight reduction as well as glucose-lowering effects mediated by glucose-dependent insulin secretion.
    MeSH term(s) Administration, Oral ; Animals ; Binding, Competitive ; Blood Glucose/analysis ; Cell Line ; Diabetes Mellitus/drug therapy ; Eating/drug effects ; Glucose Tolerance Test ; Humans ; Male ; Mice ; Mice, Inbred C57BL ; Obesity/drug therapy ; Quinazolinones/chemical synthesis ; Quinazolinones/chemistry ; Quinazolinones/pharmacology ; Radioligand Assay ; Rats ; Rats, Wistar ; Receptors, Ghrelin/antagonists & inhibitors ; Stereoisomerism ; Structure-Activity Relationship ; Weight Loss/drug effects
    Chemical Substances 6-(4-fluorophenoxy)-3-((1-isopropylpiperidin-3-yl)methyl)-2-methylquinazolin-4(3H)-one ; 6-(4-fluorophenyl)-2-isopropyl-3-((1-isopropylpiperidin-3-yl)methyl)quinazolin-4(3H)-one ; Blood Glucose ; Quinazolinones ; Receptors, Ghrelin
    Language English
    Publishing date 2007-10-18
    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/jm070071+
    Database MEDical Literature Analysis and Retrieval System OnLINE

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