Discovery of pyrazolo[4,3-c]quinolines derivatives as potential anti-inflammatory agents through inhibiting of no production

Chih Hua Tseng, Chun Wei Tung, Shin I. Peng, Yeh Long Chen, Cherng Chyi Tzeng, Chih Mei Cheng

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The synthesis and anti-inflammatory effects of certain pyrazolo[4,3-c]quinoline derivatives 2a–2r are described. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Among them, 3-amino-4-(4-hydroxyphenylamino)- 1H-pyrazolo[4,3-c]-quinoline (2i) and 4-(3-amino-1H-pyrazolo[4,3-c]quinolin-4-ylamino)benzoic acid (2m) exhibited significant inhibition of LPS-stimulated NO production with a potency approximately equal to that of the positive control, 1400W. Important structure features were analyzed by quantitative structure–activity relationship (QSAR) analysis to give better insights into the structure determinants for predicting the inhibitory effects on the accumulation of nitric oxide for RAW 264.7 cells in response to LPS. In addition, our results indicated that their anti-inflammatory effects involve the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) protein expression. Further studies on the structural optimization are ongoing.

Original languageEnglish
Article number1036
JournalMolecules
Volume23
Issue number5
DOIs
Publication statusPublished - Jan 1 2018
Externally publishedYes

Keywords

  • 3-c]quinolines
  • Anti-inflammatory activity
  • Nitric oxide
  • Pyrazolo[4

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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