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Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids
Author(s) -
Mohareb Rafat M.,
Elmegeed Gamal A.,
Baiuomy Ayman R.,
Eskander Emad F.,
William Marian G.
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000366
Subject(s) - carrageenan , chemistry , anti inflammatory , pharmacology , edema , nociception , inflammation , ethanol , medicine , biochemistry , receptor
Developing new therapeutic agents that can overcome gastrointestinal injury and at the same time could lead to an enhanced anti‐inflammatory effect becomes an urgent need for inflammation patients. Thiazolyl and pyrrolyl steroids were synthesized via straight forward and efficient methods and their structures were established based on their correct elemental analysis and compatible IR, 1 H‐NMR, 13 C‐NMR, and mass spectral data. The dihydrothiazolyl‐hydrazonoprogesterone 12 and the aminopyrrolylprogesterone 16a showed anti‐inflammatory, antinociceptive, and anti‐ulcerogenic activity with various intensities. Edema were significantly reduced by both doses of tested compounds (25 and 50 mg/kg) at 2, 3, and 4 h post‐carrageenan. The high dose of compound 16a was the most effective in alleviating thermal pain. Gastric mucosal lesions, caused in the rats by the administration of ethanol or indomethacin (IND), were significantly inhibited by each of the two tested compounds. These results provide a unique opportunity to develop new anti‐inflammatory drugs which devoid the ulcerogenic liabilities associated with currently marketed drugs.