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ABSTRACT: A series of novel 3-(1H-indole-3-yl)-1H-pyrazole-5-carbohydrazide derivatives 4Ia-n, 4IIa-b and 6 were prepared by hydrazinolysis of ethyl 3-(1H-indole-3-yl)-1H-pyrazole-5-carboxylate with hydrazine hydrate in excellent yields. These new compounds were fully characterized by spectroscopic methods, and the important intermediates 3Ie, 3IIc and 3IId were further confirmed by X-ray crystallography. All the new compounds were evaluated for their cytotoxic activity against 4 human cancer cell lines by MTT method. Some of them exhibited more potent antiproliferative activity against HepG-2, BGC823 and BT474 cell lines than the positive drug 5-fluorourcail. Flow cytometry analysis showed that 4Ik and 4Il arrested the cell cycle at S phase.
European journal of medicinal chemistry 12/2011; 46(12):5868-77. · 3.27 Impact Factor
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ABSTRACT: A series of novel compounds bearing a 3-(1H-indol-3-yl)pyrazole-5-carboxylic acid nucleus were synthesized. Analytical and spectral data confirmed the structures of the new compounds. The structures of the regioisomers in this series were determined by (1)H-NMR spectra. The title compounds were evaluated for their endothelin-1 antagonist activities. In the in vitro functional assay, compounds 23, 24, 28 and 29 exhibited significant efficacy at the concentration of 1 μg/mL, and compounds 5b, 5c, 26 and 28 were as potent as the positive control bosentan at high concentration. In the experiment to assess prevention of endothelin-1-induced sudden death in mice, compound 5b showed comparable activity to bosentan, and 30 was more potent than bosentan. The final compounds were also screened for antibacterial activity against four Gram-positive and -negative bacteria. Some of the tested compounds showed weak antibacterial activity.
Archives of Pharmacal Research 03/2011; 34(3):343-55. · 1.59 Impact Factor
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ABSTRACT: A series of novel designed mexiletine derivatives and its analogs were prepared, the structures were confirmed by Nuclear Magnetic Resonance (NMR), Fourier Transform Infrared Spectroscopy (FTIR), and Electrospray Ionization-Mass Spectrometry (ESI-MS), and the enantioseparations were performed on polysaccharide-based chiral stationary phase (CSP), Chiralcel OD-H, and Chiralcel OJ-H, under normal-phase mode. The effects of the concentration of isopropanol in the mobile phase were studied, seven of the eight enantiomers got baseline separation on Chiralcel OD-H, and five of the eight enantiomers got successfully separation on Chiralcel OJ-H. The effects of structural features were also discussed.
Chirality 02/2011; 23(2):99-104. · 2.35 Impact Factor
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Yongli Du,
Qunyi Li,
Bing Xiong,
Xin Hui,
Xin Wang,
Yang Feng,
Tao Meng,
Dingyu Hu, Datong Zhang,
Mingwei Wang,
Jingkang Shen
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ABSTRACT: A novel class of non-steroidal progesterone receptor antagonists with aromatic beta-amino-ketone scaffold have been synthesized and characterized with high binding affinity and great selectivity for the cognate receptors. Among them, compound 22 was shown to be the most potent progesterone receptor antagonist in cotransfection assay and a murine model of ligand-induced decidualization.
Bioorganic & medicinal chemistry 06/2010; 18(12):4255-68. · 2.82 Impact Factor
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ABSTRACT: Two series of novel 2-butyl succinate-based Hydroxamate derivatives containing isoxazole rings were synthesized, characterized and evaluated for antibacterial activity. The synthesized compounds were found to exhibit weak to moderate inhibitory activity against Staphytlococcus aureu and Klebsiellar pneumonia in vitro. All the compounds synthesized were found to be more effective against Klebsiellar pneumonia compared to Staphytlococcus aureu.
Archives of Pharmacal Research 06/2010; 33(6):831-42. · 1.59 Impact Factor
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Chinese Journal of Chemistry 05/2009; 27(4):628 - 632. · 0.75 Impact Factor
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ABSTRACT: Storage instability is one of the serious problems that greatly restrict pesticide use. Routine checks on the composition and toxicity of 30% emulsifiable concentrates (EC) of chloramidophos (CP) during storage indicated that 78.6% of the active ingredient had decreased, whereas the anti-acetylcholinesterase (AChE) activity of the formulation was potentiated by 3.5 times. To understand the mechanism for these changes, detailed knowledge of the products present and their effects on anti-AChE potential deserves attention. It was likely that the basis for these changes was methanol, the cosolvent of CP EC, because when the purified CP was stored in methanol at 50 degrees C for 2 weeks, CP drop and toxic potentiation similar to those observed in CP EC also appeared. The major products of the CP-methanol reaction mixture were isolated and identified by HPLC and GC-MS, respectively, and their inhibitory potentials against AChE and effectiveness as potentiators were assessed. Following redetermination of the main product (O,S-dimethyl-[(2,2,2)-trichloro-1-methoxyethyl]phosphoramidothioate (MCP)) and high anti-AChE material (methamidophos), which were preconfirmed in the reaction mixture in CP EC, it was successfully demonstrated that the majority of CP in the formulation had been transformed to a new stable compound, MCP. Meanwhile, formation of another product, methamidophos, resulted in toxic potentiation.
Journal of Agricultural and Food Chemistry 02/2009; 57(3):930-7. · 2.82 Impact Factor
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ABSTRACT: A series of novel actinonin derivatives containing a benzimidazole heterocycle linked as amide isostere have been designed and synthesized. The structures of all the synthesized compounds were confirmed by analytical and spectroscopic methods. All the compounds were evaluated in vitro against Staphylococcus aureus, Klebsiella pneumoniae, and Sarcina lutea. Among them, compound 1a with unsubstituted benzimidazole ring exhibited potent antibacterial activities.
European journal of medicinal chemistry 06/2008; 44(5):2202-10. · 3.27 Impact Factor
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ABSTRACT: The binding modes of a series of known activity inhibitors docking to Peptide deformylase (PDF) have been studied using molecular docking software AutoDock3.0.5. In this study, good correlation (R(2)=0.894) between calculated binding energies and experimental inhibitory activities is obtained. We find that some shallow pockets near the known active pocket are very important which can accommodate the side-chains of the inhibitor. Moreover, a new binding pocket is also explored. All these may provide something useful for designing the potent inhibitors.
Biophysical Chemistry 07/2006; 122(1):43-9. · 2.20 Impact Factor
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ABSTRACT: In this study, the chiral stationary phase was prepared by bonding vancomycin to 5 microm spherical silica gel according to "one-pot" synthetic strategies, and used to separate the enantiomers of zolmitriptan under polar ionic mode. The influences of mobile phase composition, such as the concentration and ratio of glacial acetic acid (HOAc) and triethylamine (TEA), on the enantioseparation were investigated, and the chiral recognition mechanism is discussed. It was found experimentally that the retention factors were increased with the increase of the HOAc/TEA concentration in a certain extent, and the ionic interactions, hydrogen bondings, and steric interactions may play key role together. The method is suitable for baseline separation of zolmitriptan enantiomers.
Journal of Separation Science 01/2006; 28(18):2501-4. · 2.73 Impact Factor
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ABSTRACT: Optically active tartaric acid and its diester derivatives are well known as effective chiral selectors. In the current studies, a self-prepared diester of tartaric acid (2R, 3R)-di-n-propyl tartrate (DPT) was used as a chiral mobile-phase additive (CMPA) for the enantioseparation of seven kinds of alkyl tropate on a silica gel column by high performance liquid chromatography (HPLC). Four kinds of alkyl tropate were successfully enantioseparated using this chiral system, indicating that DPT is a novel useful chiral selector. The influences of mobile-phase composition and solute structure on enantioseparation were extensively studied. Although different types of alcoholic additive or various concentrations of alcoholic additive, DPT and dichloromethane in the mobile phase had great influence on the retention factor (k′) and resolution (Rs), the mobile-phase composition essentially had no effect on the separation factor (α). In contrast, the structure of alkyl tropate greatly influenced the separation factor (α). The results revealed that an increase in the bulkiness of the O-alkyl groups of tropic acid esters reduced the separation factors (α), indicating that inhibition of the formation of effective hydrogen-bond interaction between DPT and solutes by the bulkiness of the O-alkyl group decreases the retentivity difference between the transient diasterieomeric complex pairs. Our observations suggested that the hydrogen-bond interactions between chiral additives and solutes might be the major chiral recognition mechanism for DPT as CMPA.
Analytica Chimica Acta. 536:15-20.
