Browsing by Author "William M.G."

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Evaluation of anti-inflammatory, anti-nociceptive, and anti-ulcerogenic activities of novel synthesized thiazolyl and pyrrolyl steroids
(2011) Mohareb R.M.; Elmegeed G.A.; Baiuomy A.R.; Eskander E.F.; William M.G.; Organic Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Elwahaat Road; October City; Egypt; Chemistry Department; Faculty of Science; Cairo University; Cario; Egypt; Hormones Department; National Research Centre; 12622 Dokki; Cairo; Egypt; Pharmacology Department; National Research Centre; Dokki; Cairo; Egypt; Faculty of Medicine and Medical Sciences; Taif University; Saudi Arabia
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, 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.
Synthesis of modified steroids as a novel class of non-ulcerogenic, anti-inflammatory and anti-nociceptive agents
(2011) Mohareb R.M.; Elmegeed G.A.; Abdel-Salam O.M.E.; Doss S.H.; William M.G.; Organic Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Elwahaat Road; October City; Egypt; Chemistry Department; Faculty of Science; Cairo University; Cario; Egypt; Hormones Department; National Research Centre; 12622 Dokki; Cairo; Egypt; Toxicology and Narcotics Department; National Research Centre; 12622 Dokki; Cairo; Egypt
The identification of compounds able to treat both pain and inflammation with limited side effects is one of the prominent goals in biomedical research. This study aimed at the synthesis of new modified steroids with structures justifying non-ulcerogenic, anti-inflammatory and anti-nociceptive activities. The steroid derivatives were synthesized via straightforward and efficient methods and their structures were established based on the analytical and spectral data. The in vivo anti-inflammatory, anti-nociceptive and anti-ulcerogenic activities of some of these compounds were studied. The newly synthesized compounds 8b, 19b, 24 and 31a showed anti-inflammatory, anti-nociceptive and anti-ulcerogenic activity with various intensities. Oedema was significantly reduced by either dose 25 or 50 mg/kg of all tested compounds at 3 and 4 h post-carrageenan. Compound 19b was the most effective in alleviating thermal pain. The analgesic activity of either dose of the compounds 8b, 24, 31a as well as the high dose 19b was significantly higher than that for indomethacin (IND). Gastric mucosal lesions caused in the rats by the administration of 96% EtOH and IND were inhibited by all tested compounds administered at (50 mg/kg) dose in the study. � 2011 Elsevier Inc. All rights reserved.