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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.
Studies on the Anti-Inflammatory and Analgesic Effects ofExtracts from Marine Sponges
Issa M.I. Fakhr,Nehal A. Hamdy,Mohamed A.A. Radwan,Seham A. El-Batran,Osama A. El Shabrawy 한국생약학회 2006 Natural Product Sciences Vol.12 No.2
specimens of sponges collected from Red Sea, Egypt, were investigated f or their contents ofsecondary metabolites. The crude extracts of the sponges were tested for their anti-inflammatory and analgesiceffects. The toxic effects of the extracts of the two marine sponges were studied. LD50 determination revealed thatthe investigated extracts of ‘Igernella and Ircinia spp’ were 4.69 and 134.7mg/100g b.wt., respectively, whentwo marine sponges extracts showed significant anti-inflamatory and analgesic eff ects. Keywordsanti-inflammatory, analgesic, sponges, Igernella, Ircinia
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.
Synthesis and Some Reactions of New Thieno[2,3-c]pyridazine Derivatives
Bakhite, Etify A.,Mohamed, Omima S.,Radwan, Shaban M. Korean Chemical Society 2002 Bulletin of the Korean Chemical Society Vol.23 No.12
Treatment of ethyl 5-hydroxy-3,4-diphenylthieno[2,3-c]pyridazine-6-carboxylate (1a) with hydrazine hydrate in ethanol gave the carbohydrazide 2,. Some derivatives of the latter compound have been synthesized. Also, 6-acetyl-3,4-diphenyl-5-hydroxythieno[2.3-c]pyridazine (1b) was subjected to some reactions to produce other new thienopyridazine derivatives.
C-Flavonoidal Glycosides from Erythrina caffra Flowers
Sawsan El Masry,Hala M. Hammoda,Mohamed M. Radwan,Samir A. Ross,Hala H. Zaatout 한국생약학회 2010 Natural Product Sciences Vol.16 No.4
A phytochemical investigation of the ethanolic extract of Erythrina caffra flowers from an Egyptian origin yielded three C-flavonoidal glycosides; 5,7,4`-trihydroxyflavone-8-C-β-D-glucopyranoside (vitexin) (1), 5,7,4`-trihydroxyflavone-6-C-β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside (isovitexin-2``-β-D-glucopyranoside) (2), 5, 7, 4`-trihydroxyflavone-6, 8-di-C-β-D-glucopyranoside (vicenin-2) (3) and one O-flavonoidal glycoside; kaempferol-3-O-β-D-glucopyranosyl) (1→2)-β-D-glucopyranoside (4). The structures of the isolated compounds (1 - 4) were elucidated using different spectral techniques (UV, 1D and 2D NMR and HRESIMS). This is the first report for the isolation of flavonoidal glycosides from Erythrina caffra. The antibacterial, antifungal, antimalarial, and antileishmanial activities of the isolates were evaluated. In addition, the cytotoxic activity of the ethanolic extract and the main fractions were tested using brine shrimp bioassay.
Clinical and Prognostic Features of Erionite-Induced Malignant Mesothelioma
Ersin Demirer,Elamin M. Elamin,Christian F. Ghattas,Mohamed O. Radwan 연세대학교의과대학 2015 Yonsei medical journal Vol.56 No.2
This review analytically examines the published data for erionite-related malignantpleural mesothelioma (E-MPM) and any data to support a genetically predisposedmechanism to erionite fiber carcinogenesis. Adult patients of age ≥18 years with erionite-related pleural diseases and genetically predisposed mechanisms to erionite carcinogenesis were included, while exclusion criteria included asbestos- or tremolite-related pleural diseases. The search was limited to human studies though not limited to a specific timeframe. A total of 33 studies (31042 patients) including 22 retrospective studies, 6 prospective studies, and 5 case reports were reviewed. E-MPM developed in some subjects with high exposures to erionite, though not all. Chest CT was more reliable in detecting various pleural changes in E-MPM than chest X-ray, and pleural effusion was the most common finding in E-MPM cases, by both tests. Bronchoalveolar lavage remains a reliable and relatively less invasivetechnique. Chemotherapy with cisplatin and mitomycin can be administered either alone or following surgery. Erionite has been the culprit of numerous malignantmesothelioma cases in Europe and even in North America. Erionite has a higher degree of carcinogenicity with possible genetic transmission of erionite susceptibilityin an autosomal dominant fashion. Therapeutic management for E-MPM remains very limited, and cure of the disease is extremely rare.
Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity
Fathalla, O.A.,Zaghary, W.A.,Radwan, H.H.,Awad, S.M.,Mohamed, M.S. The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.3
2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.