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        Synthesis and Three-dimensional Qualitative Structure Selectivity Relationship of 3,5- Disubstituted-2,4-Thiazolidinedione Derivatives As COX2 Inhibitors

        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.

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        Antifungal Activity of Green and Chemically Synthesized ZnO Nanoparticles against Alternaria citri, the Causal Agent Citrus Black Rot

        Hazem S. Elshafie(Hazem S. Elshafie ),Ali Osman(Ali Osman ),Mahmoud M El-Saber(Mahmoud M El-Saber ),Ippolito Camele(Ippolito Camele ),Entsar Abbas(Entsar Abbas ) 한국식물병리학회 2023 Plant Pathology Journal Vol.39 No.3

        Citrus black rot is a serious disease of citrus plants caused by Alternaria citri. The current study aimed to synthesize zinc oxide nanoparticles (ZnO-NPs) by chemically or green method and investigate their anti-fungal activity against A. citri. The sizes of synthesized as measured by transmission electron microscope of ZnO-NPs were 88 and 65 nm for chemical and green methods, respectively. The studied prepared ZnO-NPs were applied, in vitro and in situ, at different concen-trations (500, 1,000, and 2,000 μg/ml) in post-harvest treatment on navel orange fruits to verify the possible control effect against A. citri. Results of in vitro assay demonstrated that, at concentration 2,000 μg/ml, the green ZnO-NPs was able to inhibit about 61% of the fungal growth followed by 52% of chemical ZnO-NPs. In addition, scanning electron microscopy of A. citri treated in vitro with green ZnO-NPs showed swelling and deformation of conidia. Results showed also that, using a chemically and green ZnO-NPs at 2,000 μg/ml in situ in post-harvest treatment of orange, artificially-infected with A. citri, has reduced the disease severity to 6.92% and 9.23%, respectively, compared to 23.84% of positive control (non-treated fruits) after 20 days of storage. The out findings of this study may contribute to the development of a natural, effective, and eco-friendly strategy for eradicating harmful phytopatho-genic fungi.

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