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Molecules 2018, 23(5), 1036; https://doi.org/10.3390/molecules23051036

Discovery of Pyrazolo[4,3-c]quinolines Derivatives as Potential Anti-Inflammatory Agents through Inhibiting of NO Production

1
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
2
Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
3
Center for Infectious Disease and Cancer Research, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
4
Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung City 807, Taiwan
5
Ph.D. Program in Toxicology, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
6
Department of Medicinal and Applied Chemistry, College of Life Science, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
7
Department of Biomedical Science and Environmental Biology, College of Life Science, Kaohsiung Medical University, Kaohsiung City 807, Taiwan
*
Authors to whom correspondence should be addressed.
Academic Editor: George Kokotos
Received: 16 April 2018 / Revised: 25 April 2018 / Accepted: 27 April 2018 / Published: 28 April 2018
(This article belongs to the Section Medicinal Chemistry)
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Abstract

The synthesis and anti-inflammatory effects of certain pyrazolo[4,3-c]quinoline derivatives 2a2r 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, 1400 W. 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. View Full-Text
Keywords: pyrazolo[4,3-c]quinolines; nitric oxide; anti-inflammatory activity pyrazolo[4,3-c]quinolines; nitric oxide; anti-inflammatory activity
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Tseng, C.-H.; Tung, C.-W.; Peng, S.-I.; Chen, Y.-L.; Tzeng, C.-C.; Cheng, C.-M. Discovery of Pyrazolo[4,3-c]quinolines Derivatives as Potential Anti-Inflammatory Agents through Inhibiting of NO Production. Molecules 2018, 23, 1036.

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