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2000
Volume 12, Issue 7
  • ISSN: 1570-1808
  • E-ISSN: 1875-628X

Abstract

Various bioisosteres of ethyl pyruvate (EP), where the oxygen atom in the ethoxy group was replaced by the corresponding bioisosteric atom such as carbon, nitrogen, and sulfur atoms, were synthesized and their inhibitory effects were tested for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in lipopolysaccharide (LPS)-induced BV2 cells. The synthesized compounds generally revealed better activity than EP. Especially, the thio-bioisostere 4c (IC50 = 3.6 μM) exhibited a potency about 4.5 times greater than that of EP (IC50 = 16.1 μM) and suppressed NO production dose-dependently without cytotoxicity. Compound 4c also inhibited iNOS expression in LPS-induced BV2 cells at 1 μM and 10 μM concentrations. These results suggested that the ethoxy group in EP is not essential for the suppression of NO production and that 4c has potential as a potent inhibitor of NO production.

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/content/journals/lddd/10.2174/1570180812999150225112225
2015-08-01
2025-06-28
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/content/journals/lddd/10.2174/1570180812999150225112225
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  • Article Type:
    Research Article
Keyword(s): bioisosteres; BV2 cell; Ethyl pyruvate; inhibitor; microglia; nitric oxide
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