• Title/Summary/Keyword: Thiazole-5-carboxamide

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Synthesis of 2-(3'-azido-and 3'-amino-3'-deoxy-$\beta$-D-ribofuranosyl)-thiazole-4- carboxamide

  • Shin, Ji-Hye;Liang, Cheng-Wu;Chun, Moon-Woo
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.184.3-185
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    • 2003
  • Inosine 5'-monophosphate dehydrogenase (IMPDH) is a critical enzyme in the regulation of cell proliferation and differentiation. This enzyme catalyzes the $NAD^+$-dependent oxidation of IMP to XMP, the rate limiting step in de novo biosynthesis of guanine nucleotides. Therefore, the biochemical effect of IMPDH inhibition in sensitive cell types is decrease in intracellular guanine nucleotide levels, and the decrease in cellular GTP and deoxy GTP pool levels blocks DNA and RNA synthesis in rapidly proliferating tumor cells. (omitted)

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Biotransformation of a Fungicide Ethaboxam by Soil Fungus Cunninghamella elegans

  • PARK, MI-KYUNG;KWANG-HYEON LIU;YOONGHO LIM;YOUN-HYUNG LEE;HOR-GIL HUR;JEONG-HAN KIM
    • Journal of Microbiology and Biotechnology
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    • v.13 no.1
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    • pp.43-49
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    • 2003
  • Metabolism of a new fungicide ethaboxam by soil fungi was studied. Among the fungi tested, Cunninghamelia elegans produced metabolites from ethaboxam, which were not found in the control experiments. M5, a major metabolite from ethaboxam was firmly identified as N-deethylated ethaboxam by LC/MS/MS and NMR. N-Deethylated ethaboxam has been found as a single metabolite in in vitro metabolism with rat liver microsomes. Ml was proved to be 4-ethyl-2-(ethylamino)-1,3-thiazole-5-carboxamide (ETC) by comparing with the authentic compound. In addition, M2, M3, and M4, and M6 were tentatively Identified by LC/MS/MS as hydroxylated and methoxylated ethaboxams, respectively. Production of the major metabolite, N-deethylated ethaboxam, by the fungus suggested that C. elegans would be an efficient eukaryotic microbial candidate for evaluating xenobiotic-driven mammalian risk assessment.