Next Article in Journal
Validation of a Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Trimethoprim and Sulfadimethoxine Sodium in Oral Liquid Dosage Form
Previous Article in Journal
Feed Forward Artificial Neural Network: Tool for Early Detection of Ovarian Cancer
Article Menu

Article Versions

Export Article

Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2015). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
Open AccessArticle
Sci. Pharm. 2011, 79(3), 507-524; https://doi.org/10.3797/scipharm.1105-14 (registering DOI)

Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents

1
Department of Chemistry, Faculty of Women for Arts, Science and Education, Ain Shams University, Cairo, Egypt
2
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
3
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt
4
Department of Pharmacology & Toxicology, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo 11884, Egypt
*
Author to whom correspondence should be addressed.
Received: 19 May 2011 / Accepted: 3 July 2011 / Published: 3 July 2011
Download PDF [383 KB, uploaded 28 September 2016]

Abstract

A series of chalcone-based diarylpyrazoles containing a phenylsulphone or carbonitrile moiety was synthesized. Thus, 3-acetylpyrazoles 6a–c and 10a–c were used as useful substrates in facile synthesis of functional pyrazoles 7a–f and 11a–f, respectively. The anti-inflammatory activity and ulcerogenic effect were evaluated and some of the obtained products possessed a significant anti-inflammatory activity. 1-[1-(3-Methylphenyl)-5-phenyl-4-(phenylsulfonyl)-1H-pyrazol-3-yl]ethanone (6b) showed a high activity when compared with indomethacin as reference drug with lower gastrointestinal (GI) profile. Furthermore, molecular docking studies were performed in order to rationalize the obtained biological results.
Keywords: Diarylpyrazoles; Sulphones; Chalcones; Anti-inflammatory activity; Molecular docking Diarylpyrazoles; Sulphones; Chalcones; Anti-inflammatory activity; Molecular docking
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).

Share & Cite This Article

MDPI and ACS Style

NASSAR, E.; ABDEL-AZIZ, H.A.; IBRAHIM, H.S.; MANSOUR, A.M. Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents. Sci. Pharm. 2011, 79, 507-524.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top