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Volumn 13, Issue 17, 2003, Pages 2895-2898

Identification of a novel class of orally active pyrimido[5,4-3][1,2,4] triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; DIAMINE DERIVATIVE; PROTEIN TYROSINE PHOSPHATASE; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; TRIAZINE DERIVATIVE;

EID: 10744220924     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00623-1     Document Type: Article
Times cited : (53)

References (28)
  • 6
    • 0027569865 scopus 로고    scopus 로고
    • (b) Goldstein B.J. Receptor. 3:1993;1
    • (1993) Receptor , vol.3 , pp. 1
  • 7
    • 0028932005 scopus 로고
    • (a) Goldstein B.J. J. Cell. Biochem. 31:1992;33 (b) Goldstein B.J. Receptor. 3:1993;1 (c) Ahmad F., Goldstein B.J. Biochim. Biophys. Acta. 1248:1995;57.
    • (1995) Biochim. Biophys. Acta , vol.1248 , pp. 57
    • Ahmad, F.1    Goldstein, B.J.2
  • 15
    • 0031919553 scopus 로고    scopus 로고
    • (a) Huyer G., Liu S., Kelly J. J. Biol. Chem. 272:1997;843 (b) Tsiani E., Fantus G. Trends Endocrinol. Metab. 8:1997;51 (c) Posner B.I., Faure R., Burgess J.W., Bevan A.P., Lachance D., Zhang-Sun G., Fantus I.G., Ng J.B., Hall D.A., Lum B.S. J. Biol. Chem. 269:1994;4596 (d) Yale J.F., Lachance D., Bevan A.P., Vigeant C., Shaver A., Posner B.I. Diabetes. 44:1995;1274 (e) Halberstan M., Cohen N., Shlimovich P., Rosetti L., Shamoon H. Diabetes. 45:1996;659 (f) Fantus I.G., Tsiani E. Mol. Cell. Biochem. 182:1998;109.
    • (1998) Mol. Cell. Biochem. , vol.182 , pp. 109
    • Fantus, I.G.1    Tsiani, E.2
  • 17
    • 85030945304 scopus 로고    scopus 로고
    • 3CN gradient, lyophilized and isolated as their trifluoroacetate salts.
  • 18
    • 0028273420 scopus 로고    scopus 로고
    • m for each enzyme and 37.5 mM diethylglutarate pH 6.2 was used in place of MES. The reaction was stopped with KOH and the fluorescence of the dephosphorylated substrate measured (excitation: 360 nM/emission: 460 nM).
  • 21
    • 85030952249 scopus 로고    scopus 로고
    • 6, two NH protons could be detected at 6.93 and 8.73 ppm. Mass spectrometry revealed a species whose mass is 2 units higher than parent 16, corresponding to the addition of hydrogen and consistent with the structure 17.
  • 23
    • 85030948532 scopus 로고    scopus 로고
    • Unpublished results. A detailed account of this work will be published separately
    • Olivier, A. R. Unpublished results. A detailed account of this work will be published separately.
    • Olivier, A.R.1
  • 27
    • 85030948550 scopus 로고    scopus 로고
    • As determined by C, H, N, O, F combustion analysis, the trifluoroacetate salt of compounds 12 and 13 contains 3 mol of TFA per mol of parent 12 and 13. Thus a 50-mg/kg dose of 12 corresponds to 28 mg/kg of parent drug.
  • 28
    • 85030937600 scopus 로고    scopus 로고
    • Preliminary toxicological data was obtained following the 5 day dosing study in ob/ob mice (Table 3). No significant adverse treatment related effects were observed on organ weights, hematological parameters or serum chemistries. A histopathological evaluation of selected tissues was performed and no treatment related microscopic changes were observed.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.