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Arzneimittelforschung 2005; 55(12): 738-743
DOI: 10.1055/s-0031-1296923
Analgesics · Anti-inflammatories · Antiphlogistics · Antirheumatic Drugs
Editio Cantor Verlag Aulendorf (Germany)

Synthesis and Pharmacological Evaluation of Novel Quinoxalines as Potential Nonulcerogenic Anti-inflammatory and Analgesic Agents

Magda M. F. Ismail
a   Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, Egypt
,
Yousry A. Ammar
b   Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, Egypt
,
Mohamed K. Ibrahim
c   Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
,
Heba S. A. El-Zahaby
a   Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, Egypt
,
Sawsan S. Mahmoud
d   Pharmacology Department, National Research Centre, Cairo, Egypt
› Author Affiliations
Further Information

Publication History

Publication Date:
23 December 2011 (online)

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Summary

Some new substituted quinoxaline and furo[2,3-b]quinoxaline derivatives have been synthesized and tested for their anti-inflammatory and analgesic activities and for their ulcerogenic potential. The pharmacological evaluation of selected synthesized compounds revealed that 5a was equipotent and compounds 3, 4b, 4e and 5b possessed strong anti-inflammatory activity in chronic inflammatory models compared with indometacin (CAS 53-86-1) as reference drug. In addition, compound 4a was the safest one and the others showed little ulcerogenic activity. All the tested compounds showed moderate analgesic activity compared to the reference drug.

Zusammenfassung

Synthese und parmakologische Bewertung neuer Chinoxalin-Derivate als potentielle nichtulzerogene entzündungshemmende und schmerzlindernde Wirkstoffe

Eine Anzahl neuer substituierter Chi-noxalin- und Furo[2,3-b]chinoxalin-Derivate wurde synthetisiert und auf entzü-dungshemmende und analgetische sowie auf ulzerogene Wirkung geprüft. In Modellen chronischer Entzündung wurde festgestellt, daβ im Vergleich zur Referenzsubstanz Indometacin (CAS 53-86-1) die Verbindung 5a gleichwertig war, während 3, 4b, 4e und 5b stärkere Hemmwirkung zeigten. Die Substanz 4a war die sicherste Verbindung, die anderen zeigten schwache ulzerogene Effekte. Alle untersuchten Substanzen zeigten im Vergleich zur Referenzsubstanz mäβige analgeti-sche Wirkung.

Key words

Analgesics - Anti-inflammatory drugs, non-steroidal - Furoquinoxalines, antiinflammatory and analgesic activities, rat, synthesis - Quinoxalin-2-ones, antiinflammatory and analgesic activities, rat, synthesis