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Structure-based design of novel heterocyclesubstituted ATDP analogs as non-nucleoside reverse transcriptase inhibitors with improved selectivity and solubility

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Acta Pharmaceutica Sinica B 2023年第12期13卷 4906-4917页

作者： Li-Min Zhao Christophe Pannecouque Erik De Clerc Shuai Wang Fen-Er Chen Key Laboratory of Natural Resources of Changbai Mountain&Functional Molecules Ministry of EducationYanbian University College of PharmacyYanbian UniversityYanji 133002China Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Shanghai 200433China Rega Institute for Medical Research KU LeuvenLeuven B-3000Belgium

Following on our recently developed biphenyl-ATDP non-nucleoside reverse transcriptase inhibitor ZLM-66(SI=2019.80,S=1.9μg/mL),a series of novel heterocycle-substituted ATDP derivatives with significantly improved selectivity and solubility were identified by replacement of the biphenyl moiety of ZLM-66 with heterocyclic group with lower lipophilicity.Evidently,the representative analog 7w in this series exhibited dramatically enhanced selectivity and solubility(SI=12,497.73,S=4472μg/mL)in comparison with ZLM-66(SI=2019.80,S=1.9μg/mL).This new NNRTI conferred low nanomolar inhibition of wild-type HIV-1 strain and tested mutant strains(K103N,L1001,Y181C,E138K,and K103N+Y181C).The analog also demonstrated favorable safety and pharmacokinetic profiles,as evidenced by its insensitivity to CYP and hERG,lack of mortality and pathological damage,and good oral bioavailability in rats(F=27.1%).Further development of 7w for HIV therapy will be facilitated by this valuable information.

关键词： HIV-1 RT NNRTIS ATDP pyridone

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Synthesis of Some Azo Disperse Dyes from 1-Substituted 2-Hydroxy-6-pyridone Derivatives and Their Colour Assessment on Polyester Fabric

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Open Journal of Applied Sciences 2012年第1期2卷 54-59页

作者： Kurenkaka Johnson Sakoma Kasali Ademola Bello Mohammed Kabir Yakubu Department of Textile Science and Technology Ahmadu Bello University Zaria Nigeria

The synthesis of a series of 3-(p-substituted phenylazo)-6-pyridone dyes which is suitable for the dyeing of polyester fabrics, is described. Visible absorption spectra of the dyes were examined in various solvents and the compounds in solution exhibited hydrazone-common anion equilibrium. The electronic absorption spectra cover a λmax range of 404 - 464 nm in DMF at uniformly high absorption intensity between 5.33 × 104 - 8.55 × 104 lmol–1cm–1 and gave bright intense hues of yellow to orange on polyester fabrics. The colour parameters of the dyed fabrics were measured and the dyes have excellent exhaustion between 72% - 79% for polyester fabrics, more intense and of very good fastness properties on polyester fabrics. The remarkable degree of levelness and brightness after washing is indicative of good penetration and excellent affinity of these dyes for the polyester fabric.

关键词： pyridone Disperse Dye Exhaustion Carrier Polyester Fastness

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Effects of Two Anti-TNF-α Compounds: Etanercept and 5-Ethyl-1-Phenyl-2-(1H)-pyridone on Secreted and Cell-Associated TNF-α <i>In Vitro</i>

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Pharmacology & Pharmacy 2011年第4期2卷 238-247页

作者： Ken J. Grattendick James M. Nakashima Shri N. Giri 不详

Tumor necrosis factor-alpha (TNF-α) is a potent inflammatory cytokine and its exaggerated production has been implicated in acute, chronic and autoimmune inflammatory diseases. Proteinaceous and non-proteinaceous anti-TNF-α agents have been developed to reduce its circulating levels either by neutralizing, binding or inhibiting the de novo synthesis with the aim of achieving desirable therapeutic effects. In the present study, we compared the effects of a protein-based anti-TNF-α drug, etanercept, and a non-protein-based anti-TNF-α small molecule, 5-ethyl-1-phenyl-2-(1H) pyridone (5-EPP), on the LPS-stimulated secretion of TNF-α in the medium and TNF-α associated with the THP-1 cells in vitro. Both drugs had marked concentration-dependent inhibitory effects on the LPS-stimulated secretion of TNF-α. However, their effects on the LPS-stimulated cell-associated TNF-α were diametrically opposed to each other. For instance, etanercept further increased the level by up to 12-fold, whereas 5-EPP inhibited the level in a dose dependent manner. In addition, 5-EPP caused a significant reduction in the elevated level of cell associated TNF-α caused by LPS + etanercept. The differences in the levels of cell-associated TNF-α as reported in the present study may partly explain the adverse effects of some protein-based anti-TNF-α drugs including etanercept as opposed to a non-protein-based anti-TNF-α drug such as pirfenidone, a structural analogue of 5-EPP, for treatment of some TNF-α mediated diseases. It was concluded from the findings of this study that drugs which elevate the levels of cell associated-TNF-α will potentially have more adverse events even after reducing the secreted levels of TNF-α than the drugs which reduce both the secreted and cell-associated TNF-α levels.

关键词： Tumor Necrosis Factor-Alpha 5-Ethyl-1-Phenyl-2-(1H) pyridone Etanercept Cytokines

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PhlCl_(2)/NH_(4)SCN-Mediated Oxidative Regioselective Thiocyanation of Pyridin-2(1H)-ones

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Chinese Journal of Chemistry 2021年第9期39卷 2536-2546页

作者： Shanqing Tao Jiaxi Xiao Yadong Li Fengxia Sun Yunfei Du Tianjin Key Laboratory for Modern Drug Delivery&High-Efficiency School of Pharmaceutical Science and TechnologyTianjin UniversityTianjin 300072China College of Chemical and Pharmaceutical Engineering Hebei University of Science and TechnologyHebei Research Center of Pharmaceutical and Chemical EngineeringShijiazhuangHebei 050018China

The reaction of pyridin-2(1H)·ones with PhlCl_(2) and NH_(4)SCN enables an efficient regioselective thiocyanation,leading to the synthesis of the biologically interesting C5 thiocyanated 2-pyridones in good to high yields.The mechanistic pathway of this metal-free approach is postulated to involve the formation of the reactive thiocyanogen chloride from the reaction of PhlCl_(2) and NH4SCN followed with the regioselective electrophilic thiocyanation of the pyridin-2(1H)-one ring.

关键词： pyridone PhlCl_(2) Thiocyanogen chloride Regioselective Electrophilic thiocyanation

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Synthesis and insecticidal bioactivities of 2,3-dihydroimidazo[1,2-a] pyridin-5(1H)-one derivatives

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Chinese Chemical Letters 2019年第2期30卷 340-344页

作者： Letian Zhang Kun Liu Xusheng Shao Zhong Li Xiaoyong Xu Shanghai Key Laboratory of Chemical Biology School of Pharmacy East China University of Science and Technology Shanghai Collaborative Innovation Center for Biomanufacturing Technology

A novel synthesis of 2,3-dihydroimidazo[1,2-a]pyridin-5 (1H)-one 4 and its derivatives were described.Preliminary bioassays showed that some of the target compounds exhibited excellent insecticidal activities against brown planthopper (Nilaparvata lugens), cowpea aphids (Aphis craccivora) (4,5 a, 5 c, 5 g,5 h, 5 j, 5 r, 6 b, 6 e) and carmine spider mite (Tetranychus cinnabarinus (5 f, 5 s, 6 a) at 500 mg/L. Among them,compound 4 was still active against brown planthopper and cowpea aphids at 4 mg/L. The insecticidal activities were influenced by the types and position of the substituents, which provided guidance for the structure modifications.

关键词： Reaction selectivity 2,3-Dihydroimidazo[1,2-a]pyridin-5(1H)one Bicyclic pyridone Insecticidal activities Acaricidal activitiy

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Synthesis,spectroscopic properties and applications of novel N-heterocycle-containing benzotriazoles as UV absorbers

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Chinese Chemical Letters 2012年第9期23卷 1019-1022页

作者： Zhi Hua Cui Xi Dong Wang Jiang Chao Guo Wei Guo Chen Key Laboratory of Advanced Textile Materials and Manufacturing Technology Ministry of Education of ChinaZhejiang Sci-Tech UniversityChinaHangzhou 310018 Engineering Research Center for Eco-Dyeing&Finishing of Textiles Ministry of EducationZhejiang Sci-Tech UniversityChinaHangzhou 310018

Two novel N-heterocycle-containing benzotriazole compounds, 5-（5-chloro-2-benzotriazolyl）-6-hydroxy-l,4-dimethyl-3-car- bonitrile-2-pyddone （2） and 4-（5-chloro-2-benzotdazolyl）-5-methyl-2-phenyl-3-pyrazolone （4）, were synthesized from reactant 4- chloro-2-nitroaniline via diazotization, azo coupling, reductive cyclization and acidification. Their structures were confirmed by Fr-IR, 1H NMR, mass spectroscopy and elemental analysis. Their spectral properties were investigated and compared with that of a common commercial benzotriazole UV absorber Tinuvin 326. It is found that the novel N-heterocycle-containing benzotriazole compounds exhibit sharp single peak in the range of 280-400 nm and have much higher molar extinction coefficients than that of Tinuvin 326. Their anti-UV protection properties on polyester fabric were also evaluated and compound 4 was much superior to compound 2 due to its higher exhaustion.

关键词： Benzotriazole UV absorber Pyrazolone pyridone Anti-UV protection

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