Evaluation of anti-inflammatory, anti-nociceptive, and anti-ulcerogenic activities of novel synthesized thiazolyl and pyrrolyl steroids

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorMohareb R.M.
dc.contributor.authorElmegeed G.A.
dc.contributor.authorBaiuomy A.R.
dc.contributor.authorEskander E.F.
dc.contributor.authorWilliam M.G.
dc.contributor.otherOrganic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University of Modern Sciences and Arts (MSA)
dc.contributor.otherElwahaat Road
dc.contributor.otherOctober City
dc.contributor.otherEgypt; Chemistry Department
dc.contributor.otherFaculty of Science
dc.contributor.otherCairo University
dc.contributor.otherCario
dc.contributor.otherEgypt; Hormones Department
dc.contributor.otherNational Research Centre
dc.contributor.other12622 Dokki
dc.contributor.otherCairo
dc.contributor.otherEgypt; Pharmacology Department
dc.contributor.otherNational Research Centre
dc.contributor.otherDokki
dc.contributor.otherCairo
dc.contributor.otherEgypt; Faculty of Medicine and Medical Sciences
dc.contributor.otherTaif University
dc.contributor.otherSaudi Arabia
dc.date.accessioned2020-01-25T19:58:30Z
dc.date.available2020-01-25T19:58:30Z
dc.date.issued2011
dc.descriptionScopus
dc.description.abstractDeveloping 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.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=19956&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1002/ardp.201000366
dc.identifier.doiPubMed ID 21887799
dc.identifier.issn3656233
dc.identifier.otherhttps://doi.org/10.1002/ardp.201000366
dc.identifier.otherPubMed ID 21887799
dc.identifier.urihttps://t.ly/ndLPr
dc.language.isoEnglishen_US
dc.relation.ispartofseriesArchiv der Pharmazie
dc.relation.ispartofseries344
dc.subjectAnti-inflammatoryen_US
dc.subjectAnti-nociceptiveen_US
dc.subjectNon-ulcerogenicen_US
dc.subjectPyrroleen_US
dc.subjectSteroidsen_US
dc.subjectThiazolesen_US
dc.subjectalcoholen_US
dc.subjectaminopyrrolylprogesteroneen_US
dc.subjectantiinflammatory agenten_US
dc.subjectantiulcer agenten_US
dc.subjectdihydrothiazolyl hydrazonoprogesteroneen_US
dc.subjectindometacinen_US
dc.subjectpyrrole derivativeen_US
dc.subjectthiazole derivativeen_US
dc.subjectunclassified drugen_US
dc.subjectanalgesic activityen_US
dc.subjectanimal experimenten_US
dc.subjectantiinflammatory activityen_US
dc.subjectarticleen_US
dc.subjectclinical evaluationen_US
dc.subjectcontrolled studyen_US
dc.subjectdrug activityen_US
dc.subjectdrug efficacyen_US
dc.subjectdrug megadoseen_US
dc.subjectnonhumanen_US
dc.subjectpainen_US
dc.subjectpaw edemaen_US
dc.subjectpriority journalen_US
dc.subjectraten_US
dc.subjecttreatment responseen_US
dc.subjectAnalgesicsen_US
dc.subjectAnimalsen_US
dc.subjectAnti-Inflammatory Agentsen_US
dc.subjectAnti-Ulcer Agentsen_US
dc.subjectCarrageenanen_US
dc.subjectDisease Models, Animalen_US
dc.subjectEdemaen_US
dc.subjectInflammationen_US
dc.subjectPainen_US
dc.subjectPyrrolesen_US
dc.subjectRatsen_US
dc.subjectRats, Sprague-Dawleyen_US
dc.subjectSteroidsen_US
dc.subjectStomach Ulceren_US
dc.subjectThiazolesen_US
dc.subjectUlceren_US
dc.titleEvaluation of anti-inflammatory, anti-nociceptive, and anti-ulcerogenic activities of novel synthesized thiazolyl and pyrrolyl steroidsen_US
dc.typeArticleen_US
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