Novel Benzoxazoles Containing 4-Amino-Butanamide Moiety Inhibited LPS-Induced Inflammation by Modulating IL-6 or IL-1β mRNA Expression

Jihye Yoo, Jiyoung Park, Darong Kim, Yeonjoo Huh, Hea Young Park Choo, Hyun Ae Woo

Research output: Contribution to journalArticlepeer-review

Abstract

LPS induces inflammatory cytokines, including IL-1β, IL-6, and TNF-α, and causes an inflammatory response. The development of small molecules that have suppressive effect on those inflammatory cytokines is a desirable strategy for the treatment of inflammatory diseases. We synthesized 12 novel compounds with 4-amino-N-(4-(benzo[d]oxazol-2-ylamino)phenyl)butanamide moiety and evaluated their biological activities. Among them, 4 compounds (compound 5d, 5c, 5f, 5m and synthetic intermediate 4d) showed potent inhibition activities on IL-1β and IL-6 mRNA expression in vitro. Further, in vivo activity was evaluated with two compounds (5f and 4d) and mRNA levels of IL-1β, IL-6, and TNF-α were significantly decreased without hepatotoxicity. From the in vivo and in vitro test results, we confirmed that our synthesized compounds are effective for suppression of representative inflammatory cytokines.

Original languageEnglish
Article number5331
JournalInternational Journal of Molecular Sciences
Volume23
Issue number10
DOIs
StatePublished - 1 May 2022

Keywords

  • anti-inflammatory effect
  • benzoxazole
  • IL-1β
  • IL-6
  • mRNA expression
  • small molecules
  • TNF-α

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