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        Rational Design, Synthesis, and Biological Activity of N-(1,4-Benzoxazinone)Acetamide Derivatives as Potent Platelet Aggregation Inhibitors

        Yi Xiang,Xiu-Hua Wang,Quan Yang,Jia-Lian Tan,장희재,Hua Zuo,신동수 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.2

        Inappropriate thrombus formation within blood vessels is the leading cause of mortality in the industrialized world. Platelet aggregation activated by thrombin may have close relationship with thrombosis. Based on our studies on the pharmacophoric role of 1,4-benzoxazine-3(4H)-one for desirable platelet aggregation inhibitory activity, we identified N-(4-ethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl)acetamide (BOAP-AM6) and N-(4-butyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)-2-(4-(4-fluorophenyl)piperazin-1-yl)acetamide (BOAP-AM21) as platelet aggregation inhibitors with an IC50 of 8.93 and 8.67 μM, respectively, as potent as the positive control aspirin. A combination of structure–activity relationships studies and molecular modeling revealed that the molecule BOAP-AM6 interacted with the amino acid residue TYR166 and ARG214 in the binding site of GPIIb/IIIa receptor through hydrogen bond and compound BOAP-AM21 acted on the amino acid residue ASN215 and ALA218, both through the same approach as the reported potent molecules 7a and 7b.

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        Transcriptome sequencing and analysis of sweet osmanthus (Osmanthus fragrans Lour.)

        Hong Na Mu,Liang Gui Wang,Huo Gen Li,Xiu Lian Yang,Tao Ze Sun,Chen Xu 한국유전학회 2014 Genes & Genomics Vol.36 No.6

        Osmanthus fragrans is a woody, evergreenspecies of shrubs and small trees that is extensively plantedin sub-tropical and temperate climates as an ornamentalplant in gardens and for its health benefits. The flower colorranges from ivory to orange to pink among different varietiesand even color difference during the whole blossom inthe sweet osmanthus. Sweet osmanthus is widely cultivatedthroughout China and other countries due to its prominentfragrance, colorful flowers, and medicinal properties. However, the scanty genomic resources in the Olea familyhave greatly hindered further exploration of its geneticmechanism on these economically important traits. In thisstudy, transcriptome sequencing of O. fragrans was performedusing the Illumina HighSeqTM2000 sequencingplatform. Next generation sequencing (NGS) of the transcriptomeof O. fragrans produced 31.7G of clean bases(211,266,818 clean reads) that were assembled into256,774 transcripts and 117,595 unigenes. Of them, 197and 237 candidate genes involved in fragrance and pigmentbiosynthesis respectively were identified based on functionannotation. Meanwhile, 1 unnamed protein and 468 functionalunknown genes were also identified. Furthermore,mRNA sequencing expression profiling of O. fragranswere compared to previous genes’. In summary, thiscomprehensive transcriptome dataset allows the identificationof genes associated with several major metabolicpathways and provides a useful public information platformfor further functional genomic studiesin O. fragransLour.

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