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Ahmed M. Ali,Gamal E. Saber,Nadia M. Mahfouz,Mahmoud A. El-Gendy,Awwad A. Radwan,Mohamed A.-El. Hamid 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]- 2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-l, 10o and 10p. Compounds (9a-l, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.
Ali, Ahmed M.,Saber, Gamal E.,Mahfouz, Nadia M.,EI-Gendy, Mahmoud A.,Radwan, Awwad A.,Hamid, Mohamed A.-EI. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]-2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-I, 10o and 10p. Compounds (9a-I, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.
A New Soft-Fusion Approach for Multiple-Receiver Wireless Communication Systems
Ashraf M. Aziz,Ahmed M. ElBakly,Mohamed H.A. Azeem,Gamal A. Hamid 한국전자통신연구원 2011 ETRI Journal Vol.33 No.3
In this paper, a new soft-fusion approach for multiple-receiver wireless communication systems is proposed. In the proposed approach, each individual receiver provides the central receiver with a confidence level rather than a binary decision. The confidence levels associated with the local receiver are modeled by means of soft-membership functions. The proposed approach can be applied to wireless digital communication systems, such as amplitude shift keying, frequency shift keying, phase shift keying, multi-carrier code division multiple access, and multiple inputs multiple outputs sensor networks. The performance of the proposed approach is evaluated and compared to the performance of the optimal diversity, majority voting, optimal partial decision, and selection diversity in case of binary noncoherent frequency shift keying on a Rayleigh faded additive white Gaussian noise channel. It is shown that the proposed approach achieves considerable performance improvement over optimal partial decision, majority voting, and selection diversity. It is also shown that the proposed approach achieves a performance comparable to the optimal diversity scheme.
Fars K. Alanazi,Ibrahim A. Alsarra,Gamal El-Din I. Harisa,Ahmad Maqboul,Magdi Abdel-Hamid,Steven H. Neau 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.4
The aim of this study was to investigate human erythrocytes as a carrier for targeted drug delivery of primaquine (PQ). The process of PQ loading in human erythrocytes, as well as the effect of PQ loading on the oxidative status of erythrocytes, was also studied. At PQ concentrations of 2, 4, 6, and 8 mg/mL and an incubation time of 2 h, the ratios of the concentrations of PQ entrapped in erythrocytes to that in the incubation medium were 0.515, 0.688, 0.697 and 0.788, respectively. The maximal decline of erythrocyte reduced glutathione content was observed at 8 mg/mL of PQ compared with native erythrocytes p < 0.001. In contrast, malondialdehyde and protein carbonyl were significantly increased in cells loaded with PQ (p < 0.001). Furthermore, osmotic fragility of PQ carrier erythrocytes was increased in comparison with unloaded cells. Electron microscopy revealed spherocyte formation with PQ carrier erythrocytes. PQ-loaded cells showed sustained drug release over a 48 h period. Erythrocytes were loaded with PQ successfully, but there were some biochemical as well as physiological changes that resulted from the effect of PQ on the oxidative status of drugloaded erythrocytes. These changes may result in favorable targeting of PQ-loaded cells to reticulo-endothelial organs. The relative impact of these changes remains to be explored in ongoing animal studies.