Mohareb R.M.Elmegeed G.A.Baiuomy A.R.Eskander E.F.William M.G.Organic Chemistry DepartmentFaculty of PharmacyOctober University of Modern Sciences and Arts (MSA)Elwahaat RoadOctober CityEgypt; Chemistry DepartmentFaculty of ScienceCairo UniversityCarioEgypt; Hormones DepartmentNational Research Centre12622 DokkiCairoEgypt; Pharmacology DepartmentNational Research CentreDokkiCairoEgypt; Faculty of Medicine and Medical SciencesTaif UniversitySaudi Arabia2020-01-252020-01-2520113656233https://doi.org/10.1002/ardp.201000366PubMed ID 21887799https://t.ly/ndLPrScopusDeveloping 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, 1H-NMR, 13C-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. Novel steroid hybrids incorporating the pyrrole or thiazole moiety through different linkages have been developed. The modified steroids 12 and 16a showed anti-inflammatory, anti-nociceptive, and/or non-ulcerogenic activities. These encouraging results may be of interest for finding new potent prescriptions. Copyright � 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.EnglishAnti-inflammatoryAnti-nociceptiveNon-ulcerogenicPyrroleSteroidsThiazolesalcoholaminopyrrolylprogesteroneantiinflammatory agentantiulcer agentdihydrothiazolyl hydrazonoprogesteroneindometacinpyrrole derivativethiazole derivativeunclassified druganalgesic activityanimal experimentantiinflammatory activityarticleclinical evaluationcontrolled studydrug activitydrug efficacydrug megadosenonhumanpainpaw edemapriority journalrattreatment responseAnalgesicsAnimalsAnti-Inflammatory AgentsAnti-Ulcer AgentsCarrageenanDisease Models, AnimalEdemaInflammationPainPyrrolesRatsRats, Sprague-DawleySteroidsStomach UlcerThiazolesUlcerArticlehttps://doi.org/10.1002/ardp.201000366PubMed ID 21887799