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- 검색키워드
- 저자 : Abdel-Alim M. Abdel-Alim (검색결과 4 건)
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Alaa M. Hayallah,Walid A. Elgaher,Ola I. Salem,Abdel Alim M. Abdel Alim 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.1
Methylxanthines especially theophylline have been recognized as potent bronchodilators for the relief of acute asthma for over 65 years. Recently, it was found that bacterial infection plays a role in asthma pathogenesis. Accordingly, the present work involves the synthesis of 6-(4-(un)substituted phenyl)thiazolo[2,3-f]theophyllines 2a-g and different series of 8-(1,2,4-triazol-3-ylmethylthio)theophyllines 6-9. The chemical structures of the target compounds were proved by IR, 1H NMR, 13C NMR, EI-MS and HRMS spectroscopic techniques along with elemental analyses. The bronchodilator activity of fifteen compounds was determined in vivo by acetylcholine induced bronchospasm in anaesthetized guinea pigs. Results revealed that all compounds showed moderate to good activity; in addition, five compounds exhibited a bronchodilator activity nearly similar to that of aminophylline as a standard. The antibacterial activity of all the target compounds was investigated in vitro against both Gram-positive and Gram-negative bacterial strains. Results revealed that some compounds showed more potent antibacterial activity than ampicillin as a standard. Acute toxicity study for four target compounds revealed that none of these derivatives showed significant toxicity up to 300 mg/kg. It was found that compound 8c combined both promising bronchodilator and antibacterial activities. This compound could be subjected for further investigations as a new possible candidate in the treatment of bronchial asthma.
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Enas Nashaat Amin,Abdel-Alim M. Abdel-Alim,Samia G. Abdel-Moty,Abdel-Naser A. El-Shorbagi,Mahran Sh. Abdel-Rahman 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.1
4,5-dihydro-3(2H)pyridazinones such as CI-914, CI-930 and pimobendan along with tetrahydropyridopyridazine (endralazine) and perhydropyridazinodiazepine (cilazopril) have been used as potent positive inotropes, antihypertensives as well as platelet aggregation inhibitors. Accordingly, the present work involves the synthesis of 24 target compounds; 4,5-dihydro-3(2H)pyridazinones in addition to seven reported intermediates. The chemical structures of the new compounds were assigned by microanalysis, IR, 1H-NMR spectral analysis and some representatives by mass spectrometry. The positive inotropic effect of the final compounds and the intermediates 12a-12d as well as the reported intermediate compound 10 was determined in-vitro on isolated rabbit heart in comparison to digoxin. Data obtained revealed that twelve of the test compounds exhibited higher effective response than digoxin, nine compounds elicited comparable effects to digoxin and eight compounds were less active than digoxin. In addition, four compounds approved marked significant hypotensive effect better than that of the previously reported compound 10. Moreover, two compounds induced complete platelet aggregation inhibition. The last two compounds were also subjected to determination of their LD50 and they showed no signs of toxicity up to the dose level 300 mg/kg (i.p.), while the reported oral LD50 of digoxin is 17.78 mg/kg. Correlation of cardiotonic and hypotensive activities with structures of compounds was tried and pharmacophore models were computed to get useful insight onto the essential structural features required for inhibiting phosphodiesterase-III in the heart muscles and blood vessels.
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Alaa A. K. M. Hayallah,Ahmad A. Talhouni,Alim M. Abdel Alim 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.8
Theophylline derivatives have long been recognized as potent bronchodilators for the relief of acute asthma. Recently, it was found that bacterial infection has a role in asthma pathogenesis. The present work involves the design and synthesis of 8-substituted theophylline derivatives as bronchodilators and antibacterial agents. The chemical structures of these compounds were elucidated by IR, 1H-NMR, mass spectrometry, and elemental analyses. The bronchodilator activity was evaluated using acetylcholine-induced bronchospasm in guinea pigs, and most of the compounds showed significant anti-bronchoconstrictive activity in comparison with standard aminophylline. In addition, the antibacterial activity of all the target compounds was investigated in vitro against Gram-positive and Gram-negative bacteria using ampicillin as a reference drug. Results showed that some of the tested compounds possessed significant antibacterial activity. A pharmacophore model was computed to obtain useful insight into the essential structural features of bronchodilator activity. A structure activity relationship was also discussed.
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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.
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