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Sci. Pharm. 2011, 79(3), 507-524; doi:10.3797/scipharm.1105-14

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
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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).

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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.

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