title: Evaluation of anti-inflammatory, anti-nociceptive, and anti-ulcerogenic activities of novel synthesized thiazolyl and pyrrolyl steroids.
abstract: 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.
authors: Organic Chemistry Department, October University of Modern Sciences and Arts (MSA), Egypt.
authors: Rafat M
authors: RM
authors: Mohareb
authors: Gamal A
authors: GA
authors: Elmegeed
authors: Ayman R
authors: AR
authors: Baiuomy
authors: Emad F
authors: EF
authors: Eskander
authors: Marian G
authors: MG
authors: William
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002351:Carrageenan; D004195:Disease Models, Animal; D004487:Edema / Q000188:drug therapy; D007249:Inflammation / Q000188:drug therapy; D010146:Pain / Q000188:drug therapy; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013276:Stomach Ulcer / Q000188:drug therapy / Q000473:pathology / Q000517:prevention & control; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry; D014456:Ulcer / Q000188:drug therapy
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000897:Anti-Ulcer Agents; D011758:Pyrroles; D013256:Steroids; D013844:Thiazoles; D002351:Carrageenan