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Abdel-Alim Abdel-Alim Mohamed,EI-Shorbagi Abdel-Nasser Ahmed,Abdel-Moty Samia Galal,Abdel-Allah Hajjaj Hassan Mohamed The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.6
This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prod rugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, $LD_{50}$, in vivo and in vitro metabolism of compound 7f were determined.
Butyrate regulates leptin expression through different signaling pathways in adipocytes
Mohamed Mohamed Soliman,Mohamed Mohamed Ahmed,Alaa-eldin Salah-eldin,Abeer Abdel-Alim Abdel-Aal 대한수의학회 2011 Journal of Veterinary Science Vol.12 No.4
Leptin is an adipocytokine that regulates body weight, and maintains energy homeostasis by promoting reduced food intake and increasing energy expenditure. Leptin expression and secretion is regulated by various factors including hormones and fatty acids. Butyrate is a short-chain fatty acid that acts as source of energy in humans. We determined whether this fatty acid can play a role in leptin expression in fully differentiated human adipocytes. Mature differentiated adipocytes were incubated with or without increasing concentrations of butyrate. RNA was extracted and leptin mRNA expression was examined by Northern blot analysis. Moreover, the cells were incubated with regulators that may affect signals which may alter leptin expression and analyzed with Northern blotting. Butyrate stimulated leptin expression, and stimulated mitogen activated protein kinase (MAPK) and phospho-CREB signaling in a time-dependent manner. Prior treatment of the cells with signal transduction inhibitors as pertusis toxin, Gi protein antagonist, PD98059 (a MAPK inhibitor), and wortmannin (a PI3K inhibitor) abolished leptin mRNA expression. These results suggest that butyrate can regulate leptin expression in humans at the transcriptional level. This is accomplished by: 1) Gi protein-coupled receptors specific for short-chain fatty acids, and 2) MAPK and phosphatidylinositol-3-kinase (PI3K) signaling pathways.
Abdel-Alim Mohamed Abdel-Alim,Abdel-Nasser Ahmed El-Shorbagi,Samia Galal Abdel-Moty,Hajjaj Hassan Mohamed Abdel-Allah 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.6
This work includes the synthesis of 15 final compounds (6a-h and 7b-h) as prodrugs of 5-ASA in the form of the acid itself, esters and amides linked by an amide linkage through a spacer to the endocyclic ring N of nicotinamide. Also, 15 new intermediate compounds were prepared. The target compounds (6b, 6f, 7b, and 7e-h) revealed potent analgesic and anti-inflammatory activities in comparison to sulfasalazine and 5-ASA. In addition, ulcerogenicity, LD50, in vivo and in vitro metabolism of compound 7f were determined.
Mohamed, Bahaa Gamal,Hussein, Mostafa Ahmed,Abdel-Alim, Abdel-Alim Mohamed,Hashem, Mohammed The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.1
Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.
Bahaa Gamal Mohamed,Mostafa Ahmed Hussein,Abdel-Alim Mohamed Abdel-Alim,Mohammed Hashem 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.1
Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3- a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2- alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3- a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.
Anber F. Mohammed,Samia G. Abdel-Moty,Mostafa A. Hussein,Abdel Alim M. Abdel Alim 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.12
The present work describes the synthesis andevaluation of some new acetohydrazones, 1,3,4-oxadiazolesand 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole asanti-inflamm atory-analgesic agents. Structure elucidation ofthese compounds was confirmed by IR, 1H NMR, and massspectrometry along with elemental microanalyses. Mostcompounds exhibited significant anti-inflammatory activityin comparison to indomethacin. Further, some compoundswere tested for their analgesic effects where two compoundsshowed results comparable to indomethacin at 4 h interval. The most active anti-inflammatory and analgesic compounds(4c and 11a) were examined on gastric mucosa and didn’tshow any gastric ulcerogenic effect compared with the referenceindomethacin. Moreover, LD50 of compounds (4c and11a) were determined in mice; they were found non toxic upto 240 and 300 mg/kg (i.p.). Also, docking simulation ofsome compounds into COX active sites was studied.