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  1. Article: Novel thiophenes and analogues with anthelmintic activity against Haemonchus contortus.

    González, Isabel C / Davis, Leon N / Smith, Charles K

    Bioorganic & medicinal chemistry letters

    2004  Volume 14, Issue 15, Page(s) 4037–4043

    Abstract: A new series of analogues of 4-(4-fluorophenyl)-2-methylthio-thiophene-3-carbonitrile (1) were synthesized and evaluated for their in vitro and in vivo anthelmintic activity against Haemonchus contortus. ...

    Abstract A new series of analogues of 4-(4-fluorophenyl)-2-methylthio-thiophene-3-carbonitrile (1) were synthesized and evaluated for their in vitro and in vivo anthelmintic activity against Haemonchus contortus.
    MeSH term(s) Animals ; Anthelmintics/chemical synthesis ; Anthelmintics/pharmacology ; Haemonchus/drug effects ; Kinetics ; Molecular Structure ; Structure-Activity Relationship ; Thiophenes/chemical synthesis ; Thiophenes/chemistry ; Thiophenes/pharmacology
    Chemical Substances Anthelmintics ; Thiophenes
    Language English
    Publishing date 2004-08-02
    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.2004.05.044
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
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  2. Article: Variations of 2,3-biphosphoglycerate (2,3-BPG) with oxygen therapy.

    de la Morena García, E / González Isabel, C

    Biochemical medicine

    1983  Volume 30, Issue 2, Page(s) 135–140

    MeSH term(s) Adenine Nucleotides/blood ; Adenosine Diphosphate/blood ; Adenosine Monophosphate/blood ; Adenosine Triphosphate/blood ; Aged ; Diphosphoglyceric Acids/blood ; Humans ; Male ; Myocardial Infarction/therapy ; Oxygen Inhalation Therapy ; Pneumonia/therapy
    Chemical Substances Adenine Nucleotides ; Diphosphoglyceric Acids ; Adenosine Monophosphate (415SHH325A) ; Adenosine Diphosphate (61D2G4IYVH) ; Adenosine Triphosphate (8L70Q75FXE)
    Language English
    Publishing date 1983-10
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 391807-5
    ISSN 0006-2944
    ISSN 0006-2944
    DOI 10.1016/0006-2944(83)90079-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Inhibición de la enzima colesática, 5'nucleotidasa por niveles altos de bilirrubina.

    De la Morena García, E / González Isabel, C

    Revista clinica espanola

    1981  Volume 161, Issue 4, Page(s) 233–234

    Title translation Inhibition of the cholestatic enzyme 5'-nucleotidase by high levels of bilirubin.
    MeSH term(s) 5'-Nucleotidase ; Bilirubin/blood ; Bilirubin/physiology ; Cholestasis/enzymology ; Humans ; Nucleotidases/antagonists & inhibitors
    Chemical Substances Nucleotidases (EC 3.1.3.-) ; 5'-Nucleotidase (EC 3.1.3.5) ; Bilirubin (RFM9X3LJ49)
    Language Spanish
    Publishing date 1981-05-31
    Publishing country Spain
    Document type English Abstract ; Journal Article
    ZDB-ID 123597-7
    ISSN 0014-2565 ; 0014-2565
    ISSN (online) 0014-2565
    ISSN 0014-2565
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  4. Article: In vitro and in vivo characterization of p-amino-phenethyl-m-trifluoromethylphenyl piperazine (PAPP), a novel serotonergic agonist with anthelmintic activity against Haemonchus contortus, Teladorsagia circumcincta and Trichostrongylus colubriformis.

    White, W Hunter / Gutierrez, Jesus A / Naylor, Sharon A / Cook, Carolyn A / Gonzalez, Isabel C / Wisehart, Mark A / Smith, Charles K / Thompson, William A

    Veterinary parasitology

    2007  Volume 146, Issue 1-2, Page(s) 58–65

    Abstract: The neurotransmitter serotonin (5-hydroxy tryptamine or 5HT) regulates key physiological processes in nematodes such as locomotion and feeding. PAPP (p-amino-phenethyl-m-trifluoromethylphenyl piperazine) is a known agonist of the 5-HT(1Hc) receptor of ... ...

    Abstract The neurotransmitter serotonin (5-hydroxy tryptamine or 5HT) regulates key physiological processes in nematodes such as locomotion and feeding. PAPP (p-amino-phenethyl-m-trifluoromethylphenyl piperazine) is a known agonist of the 5-HT(1Hc) receptor of the barber pole worm, Haemonchus contortus. In this study, PAPP was highly active against L3-stage larvae of H. contortus and Trichostrongylus colubriformis in an in vitro larval migration assay, with EC50 values of 9.36 and 11.8 microM, respectively, that were comparable to levamisole (10.2 microM) and superior to pyrantel (55.39 microM). When administered orally or subcutaneously to nematode infected gerbils, PAPP provided >99% efficacy against H. contortus and >98% efficacy against Teladorsagia circumcincta at 100 mg/kg, comparable to levamisole at 10 mg/kg. Drug titration revealed significant activity down to 50 mg/kg against these two species. Spectrum was limited, however, with somewhat lower efficacy (83%) in T. colubriformis infected gerbils at 100 mg/kg. Oral delivery of hydrochloride, acetate and phosphate salts of PAPP to nematode infected gerbils did not result in an increase in either potency or spectrum. The finding that PAPP exhibits significant anthelmintic activity suggests that the nematode-specific serotonergic system is a viable target for future anthelmintic discovery.
    MeSH term(s) Animals ; Anthelmintics/pharmacology ; Dose-Response Relationship, Drug ; Gerbillinae ; Larva/drug effects ; Molecular Structure ; Piperazines/chemistry ; Piperazines/pharmacology ; Trichostrongyloidea/drug effects
    Chemical Substances Anthelmintics ; Piperazines ; LY 165163 (8HAJ699EWG)
    Language English
    Publishing date 2007-05-15
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 196831-2
    ISSN 1873-2550 ; 0304-4017
    ISSN (online) 1873-2550
    ISSN 0304-4017
    DOI 10.1016/j.vetpar.2007.02.014
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Design and synthesis of a novel class of dual PPARgamma/delta agonists.

    Gonzalez, Isabel C / Lamar, Jason / Iradier, Fatima / Xu, Yanping / Winneroski, Leonard L / York, Jeremy / Yumibe, Nathan / Zink, Richard / Montrose-Rafizadeh, Chahrzad / Etgen, Gary J / Broderick, Carol L / Oldham, Brian A / Mantlo, Nathan

    Bioorganic & medicinal chemistry letters

    2007  Volume 17, Issue 4, Page(s) 1052–1055

    Abstract: The design and synthesis of dual PPAR gamma/delta agonist (R)-3-{2-ethyl-4-[3-(4-ethyl-2-pyridin-2-yl-phenoxy)-butoxy]-phenyl}propionic acid is described. This compound dose-dependently lowered plasma glucose in hyperglycemic male Zucker diabetic fatty ( ... ...

    Abstract The design and synthesis of dual PPAR gamma/delta agonist (R)-3-{2-ethyl-4-[3-(4-ethyl-2-pyridin-2-yl-phenoxy)-butoxy]-phenyl}propionic acid is described. This compound dose-dependently lowered plasma glucose in hyperglycemic male Zucker diabetic fatty (ZDF) rats and produced less weight gain relative to rosiglitazone at an equivalent level of glucose control.
    MeSH term(s) Animals ; Blood Glucose/metabolism ; Dose-Response Relationship, Drug ; Drug Design ; Female ; Half-Life ; Humans ; Hypoglycemic Agents/chemical synthesis ; Hypoglycemic Agents/pharmacokinetics ; Hypoglycemic Agents/pharmacology ; Indicators and Reagents ; Insulin/blood ; Male ; PPAR delta/agonists ; PPAR gamma/agonists ; Rats ; Rats, Sprague-Dawley ; Rats, Zucker ; Structure-Activity Relationship ; Thiazolidinediones/pharmacology ; Weight Gain/drug effects
    Chemical Substances Blood Glucose ; Hypoglycemic Agents ; Indicators and Reagents ; Insulin ; PPAR delta ; PPAR gamma ; Thiazolidinediones ; rosiglitazone (05V02F2KDG)
    Language English
    Publishing date 2007-02-15
    Publishing country England
    Document type Comparative Study ; Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2006.11.029
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Porphobilinogen synthetase activity response to increased levels of reduced glutathione produced by methylene blue, in blood, liver and kidney.

    Jerez, E / de la Piedra, C / González Isabel, C / Castro Mendoza, H J

    Biomedicine / [publiee pour l'A.A.I.C.I.G.

    1979  Volume 31, Issue 5, Page(s) 132–135

    Abstract: We have studied the effect of methylene blue on GSH and GSSG levels in rat blood, liver and kidney. Methylene blue treatment increases GSH levels and PBG-synthetase activity in erythrocytes while liver and kidney GSH and GSSG levels remain constant. ... ...

    Abstract We have studied the effect of methylene blue on GSH and GSSG levels in rat blood, liver and kidney. Methylene blue treatment increases GSH levels and PBG-synthetase activity in erythrocytes while liver and kidney GSH and GSSG levels remain constant. These results indicate that methylene blue effect on PBG-synthetase activity in rat erythrocytes is mediated by an increase in blood GSH levels.
    MeSH term(s) Animals ; Erythrocytes/metabolism ; Glutathione/blood ; Glutathione/metabolism ; Kidney/metabolism ; Liver/metabolism ; Male ; Methylene Blue/pharmacology ; Oxidation-Reduction ; Porphobilinogen Synthase/blood ; Porphobilinogen Synthase/metabolism ; Rats
    Chemical Substances Porphobilinogen Synthase (EC 4.2.1.24) ; Glutathione (GAN16C9B8O) ; Methylene Blue (T42P99266K)
    Language English
    Publishing date 1979-09
    Publishing country France
    Document type Journal Article
    ZDB-ID 185449-5
    ISSN 0300-0893 ; 0300-0885
    ISSN 0300-0893 ; 0300-0885
    Database MEDical Literature Analysis and Retrieval System OnLINE

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