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Volume 79
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Article

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

by
Ekhlass NASSAR
1,*,
Hatem A. ABDEL-AZIZ
2,
Hany S. IBRAHIM
3 and
Ahmed M. MANSOUR
4
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.
Sci. Pharm. 2011, 79(3), 507-524; https://doi.org/10.3797/scipharm.1105-14
Submission received: 19 May 2011 / Accepted: 3 July 2011 / Published: 3 July 2011
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.1105-14

AMA Style

NASSAR E, ABDEL-AZIZ HA, IBRAHIM HS, MANSOUR AM. Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents. Scientia Pharmaceutica. 2011; 79(3):507-524. https://doi.org/10.3797/scipharm.1105-14

Chicago/Turabian Style

NASSAR, Ekhlass, Hatem A. ABDEL-AZIZ, Hany S. IBRAHIM, and Ahmed M. MANSOUR. 2011. "Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents" Scientia Pharmaceutica 79, no. 3: 507-524. https://doi.org/10.3797/scipharm.1105-14

APA Style

NASSAR, E., ABDEL-AZIZ, H. A., IBRAHIM, H. S., & MANSOUR, A. M. (2011). Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents. Scientia Pharmaceutica, 79(3), 507-524. https://doi.org/10.3797/scipharm.1105-14

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