Next Article in Journal
Ethylenediamine Derived Carboxamides of Betulinic and Ursolic Acid as Potential Cytotoxic Agents
Previous Article in Journal
Applications of Ion Mobility-Mass Spectrometry in Carbohydrate Chemistry and Glycobiology
Article Menu
Issue 10 (October) cover image

Export Article

Open AccessArticle
Molecules 2018, 23(10), 2556; https://doi.org/10.3390/molecules23102556

Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE2 and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages

1
Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), Dokki, Giza 12622, Egypt
2
Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah 27272, UAE
3
Sharjah Institute for Medical Research, University of Sharjah, Sharjah 27272, UAE
4
Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt
5
Department of Chemistry, Hanseo University, Seosan 31962, Korea
6
Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 02792 Korea
7
Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 130-650, Korea
8
Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 130-650, Korea
9
Center for Biomaterials, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650, Korea
10
Department of Biomolecular Science, University of Science and Technology, Daejeon, Yuseong-gu 34113, Korea
*
Authors to whom correspondence should be addressed.
Received: 17 September 2018 / Revised: 29 September 2018 / Accepted: 2 October 2018 / Published: 7 October 2018
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [2407 KB, uploaded 13 October 2018]   |  

Abstract

This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. The IC50 for nitric oxide inhibition, PGE2 inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity. View Full-Text
Keywords: anti-inflammatory; inducible nitric oxide synthase (iNOS); nitric oxide; prostaglandine E2; triarylpyrazole anti-inflammatory; inducible nitric oxide synthase (iNOS); nitric oxide; prostaglandine E2; triarylpyrazole
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Abdel-Maksoud, M.S.; El-Gamal, M.I.; Gamal El-Din, M.M.; Choi, Y.; Choi, J.; Shin, J.-S.; Kang, S.-Y.; Yoo, K.H.; Lee, K.-T.; Baek, D.; Oh, C.-H. Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE2 and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages. Molecules 2018, 23, 2556.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top