title: Design, synthesis and anti-inflammatory activity of structurally simple anthranilic acid congeners devoid of ulcerogenic side effects.
abstract: Simple, three classes of new anthranilic acid derivatives were aimed at, synthesized and tested for their toxicity, anti-inflammatory, analgesic, antipyretic activity. Also, their potential protective role against ulcerative colitis in rats was performed. Furthermore, their effect on liver and kidney functions was detected through measurement of the serum level of alanine transaminase (ALT), aspartate aminotransferase (AST), urea, creatinine and other parameters. Compounds 4, 5, 6b, 6c, 7c and 7e showed significant anti-inflammatory activity. From those 6b and 7e best improved the inflammatory indices even producing better reduction in the intensity of lesion score, ulcer area and wet weight/length ratio and showed good analgesic activity. Fortunately, none of the tested compounds showed any hepatotoxicity or nephrotoxicity. None of the tested compounds showed any antipyretic activity. Conclusively, presence of a phenyl ring in the substituent added is a must, since any alteration in its nature led to decrease in activity. Also, the presence of an extra halogen in addition to the one already embedded in the main structure was detrimental to activity.
authors.affiliation: Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, POB 11562, Cairo, Egypt. phd_amalabdelhaleem@hotmail.com
authors.forename: Amal Abdel Haleem
authors.initials: AA
authors.lastname: Mohamed Eissa
authors.forename: Gamal Abd El-Hakeem
authors.initials: GA
authors.lastname: Soliman
authors.forename: Moayad Hussein
authors.initials: MH
authors.lastname: Khataibeh
mesh_terms: D000410:Alanine Transaminase / Q000097:blood; D000700:Analgesics / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D058633:Antipyretics / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001219:Aspartate Aminotransferases / Q000097:blood; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control; D003106:Colon / Q000473:pathology; D003401:Creatine / Q000097:blood; D007668:Kidney / Q000187:drug effects / Q000502:physiology; D007677:Kidney Function Tests; D007928:Lethal Dose 50; D008099:Liver / Q000187:drug effects / Q000502:physiology; D008111:Liver Function Tests; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D014456:Ulcer / Q000139:chemically induced; D014508:Urea / Q000097:blood; D062367:ortho-Aminobenzoates / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D058633:Antipyretics; D062367:ortho-Aminobenzoates; C031385:anthranilic acid; D014508:Urea; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase; D003401:Creatine