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Chelvi S.K.T.,National University of Singapore | Zhao J.,National University of Singapore | Chen L.,Xuzhou Medical College | Yan S.,National University of Singapore | And 5 more authors.
Journal of Chromatography A | Year: 2014

A new type of 4-isopropylcalix[4]arene-capped (3-(2-O-β-cyclodextrin)-2-hydroxypropoxy)propylsilyl-appended silica particles (IPC4CD-HPS) has been prepared by treatment of bromoacetate-substituted (3-(2-O-β-cyclodextrin)-2-hydroxypropoxy)propylsilyl-appended silica particles (BACD-HPS) with 4-isopropylcalix[4]arene oxyanions in anhydrous N-methyl-2-pyrrolidone. The bonded silica IPC4CD-HPS has been successfully used as chiral stationary phase (CSP) in high-performance liquid chromatography (HPLC) for the first time. The synthetic stationary phase was characterized by means of elemental analysis and Fourier transform infrared spectroscopy. This new CSP has a chiral selector with two anchored functional moieties: 4-isopropylcalix[4]arene and β-cyclodextrin. The chromatographic performance of IPC4CD-HPS was investigated by separation of positional isomers of several disubstituted benzenes and enantiomers of some chiral drug compounds under reversed-phase conditions. The results showed that IPC4CD-HPS had excellent selectivity for the separation of aromatic positional isomers and enantiomers of chiral compounds due to the cooperative functioning of the anchored 4-isopropylcalix[4]arenes and β-cyclodextrins. © 2013 Elsevier B.V. Source

Wang J.,Jiaxing University | Zong Q.,Jiaxing University | Wu Q.,Jiangsu Nhwa Pharmaceutical Co. | Shen J.,Jiaxing University | And 2 more authors.
Tetrahedron | Year: 2015

Three 2-cyano boron-dipyrromethene (BODIPY) based derivatives (CB1-CB3) have been synthesized and characterized. The photophysical properties of these compounds are investigated by means of UV/Vis absorption and fluorescence spectroscopy. CB1-CB3 exhibit small Stokes shift and high fluorescence quantum yield. Noticeably, CB2 with styrene moieties at 5-position of BODIPY displays absorption alternation with maximum of 120 nm red-shift upon addition of DBU (1,8-diazabicyclo[5.4.0]undec-7-ene) as a base, giving remarkable color change which can be detected by naked eye. Meanwhile, the compound CB3 shows high selectivity toward fluoride ion via fluorescence quenching mechanism by release of the masked phenolate form of CB2 through fluoride ion induced deprotection reaction. It also exhibits fast signal response time (30 s) and excellent selectivity over other competing analytes, making it a good candidate as colorimetric sensor for fluoride sensing. © 2015 Elsevier Ltd. Source

Chen Y.,Huazhong University of Science and Technology | Xu X.,Jiangsu Nhwa Pharmaceutical Co. | Liu X.,Huazhong University of Science and Technology | Yu M.,Jiangsu Nhwa Pharmaceutical Co. | And 3 more authors.
PLoS ONE | Year: 2012

Background: It is important to develop novel antipsychotics that can effectively treat schizophrenia with minor side-effects. The aim of our work is to develop novel antipsychotics that act on dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors with low affinity for the serotonin 5-HT2C and H1 receptors, which can effectively cure positive symptoms, negative symptoms and cognitive impairment without the weight gain side-effect. Methodology/Principal Findings: A series of 2-substituted-5-thiopropylpiperazine (piperidine) -1,3,4-oxadiazoles derivatives have been synthesized and the target compounds were evaluated for binding affinities to D2, 5-HT1A and 5-HT2A receptors. Preliminary results indicated that compounds 14, 16 and 22 exhibited high affinities to D2, 5-HT1A and 5-HT2A receptors among these compounds. Further binding tests showed that compound 22 had high affinity for D3 receptor, and low affinity for serotonin 5-HT2C and H1 receptors. In addition, compound 22 inhibited apomorphine-induced climbing behavior and MK-801-induced hyperactivity with no extrapyramidal symptoms liability in mice. Moreover, compound 22 exhibited acceptable pharmacokinetic properties. Conclusions/Significance: Compound 22 showed an atypical antipsychotic activity without liability for extrapyramidal symptoms. We anticipate compound 22 to be useful for developing a novel class of drug for the treatment of schizophrenia. © 2012 Chen et al. Source

Zhang H.,Huazhong University of Science and Technology | Xu X.,Jiangsu Nhwa Pharmaceutical Co. | Chen Y.,Jiangsu Nhwa Pharmaceutical Co. | Qiu Y.,Jiangsu Nhwa Pharmaceutical Co. | And 4 more authors.
PLoS ONE | Year: 2014

Background: Soft drugs are molecules that are purposefully designed to be rapidly metabolized (metabolically labile). In anesthesia, the soft drug is useful because it enables precise titration to effect and rapid recovery, which might allow swift and clear-headed recovery of consciousness and early home readiness. Propofol may cause delayed awakening after prolonged infusion. Propanidid and AZD3043 have a different metabolic pathway compared to propofol, resulting in a short-acting clinical profile. Fluorine imparts a variety of properties to certain medicines, including an enhanced absorption rate and improved drug transport across the blood-brain barrier. We hypothesized that the introduction of fluorine to the frame structure of propanidid and AZD3043 would further accelerate the swift and clear-headed recovery of consciousness. To test this hypothesis, we developed a series of fluorine-containing phenyl acetate derivatives. Methodology/Principal Findings: Fluorine-containing phenyl acetate derivatives were synthesized, and their hypnotic potencies and durations of LORR following bolus or infusion administration were determined in mice, rats and rabbits. The metabolic half-lives in the blood of various species were determined chromatographically. In vitro radioligand binding and γ-aminobutyric acidA (GABAA) receptor electrophysiology studies were performed. Among the 12 synthesized fluorine-containing phenyl acetate derivatives, compound 5j induced comparable duration of LORR with AZD3043, but more rapid recovery than AZD3043, propanidid and propofol. The time of compound 5j to return to walk and behavioral recovery are approximately reduced by more than 50% compared to AZD3043 in mice and rats and rabbits. The HD50 of compound 5j decreased with increasing animal size. Conclusions/Significance: The rapid recovery might make compound 5j suitable for precise titration and allow swift and clear-headed recovery of consciousness and early home readiness. © 2014 Zhang et al. Source

Wang S.,Huazhong University of Science and Technology | Chen Y.,Jiangsu Nhwa Pharmaceutical Co. | Zhao S.,Jiangsu Nhwa Pharmaceutical Co. | Xu X.,Jiangsu Nhwa Pharmaceutical Co. | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

A series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b][1,4]dioxine derivatives (5a-5d and 8a-8j) was synthesized. Compounds were evaluated for binding affinities at the 5-HT1A and 5-HT2A receptors. Antidepressant activities of the compounds were screened using the forced swimming test (FST) and the tail suspension test (TST). The results indicated that the compounds exhibited high affinities for the 5-HT1A and 5-HT2A receptors and showed a marked antidepressant-like activity. Compound 8g exhibited high affinities for the 5-HT1A (Ki = 17 nM) and 5-HT2A (Ki = 0.71 nM) receptors; it also produced a decrease of the immobility time and exhibited potent antidepressant-like effects in the FST and TST in mice. © 2014 Elsevier Ltd. All rights reserved. Source

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