The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Ying-yeung Yeung - One of the best experts on this subject based on the ideXlab platform.
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synthesis of macrocyclic ketones through catalyst free electrophilic halogen mediated semipinacol rearrangement application to the total synthesis of Muscone
Organic Letters, 2017Co-Authors: Yi Liu, Ying-yeung YeungAbstract:A series of macrocycles were successfully prepared using electrophilic halogen-mediated semipinacol rearrangement under mild conditions. Although the expansion from small ring to medium ring is an energetically unfavorable process, the electrophilic halogenation was found to be powerful enough to override such an energy barrier. The rearranged products could further undergo Dowd–Beckwith rearrangement to give the corresponding one-carbon ring-expanded ketones. This approach has been applied to the total synthesis of the natural product (±)-Muscone, which is widely used in modern perfumery and medicines, in a two-step sequence.
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Synthesis of Macrocyclic Ketones through Catalyst-Free Electrophilic Halogen-Mediated Semipinacol Rearrangement: Application to the Total Synthesis of (±)-Muscone
2017Co-Authors: Yi Liu, Ying-yeung YeungAbstract:A series of macrocycles were successfully prepared using electrophilic halogen-mediated semipinacol rearrangement under mild conditions. Although the expansion from small ring to medium ring is an energetically unfavorable process, the electrophilic halogenation was found to be powerful enough to override such an energy barrier. The rearranged products could further undergo Dowd–Beckwith rearrangement to give the corresponding one-carbon ring-expanded ketones. This approach has been applied to the total synthesis of the natural product (±)-Muscone, which is widely used in modern perfumery and medicines, in a two-step sequence
Shuang Wang - One of the best experts on this subject based on the ideXlab platform.
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self assembled thermoresponsive nanogels prepared by reverse micelle positive micelle method for ophthalmic delivery of Muscone a poorly water soluble drug
Journal of Pharmaceutical Sciences, 2016Co-Authors: Guohua Wang, Chen Zang, Baoxian Zhang, Shuang WangAbstract:Abstract This study aimed to design a nanocarrier ophthalmic delivery system of Muscone, a poorly water-soluble drug. The Muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high Muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is P app ). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of Muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.
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self assembled thermoresponsive nanogels prepared by reverse micelle positive micelle method for ophthalmic delivery of Muscone a poorly water soluble drug
Journal of Pharmaceutical Sciences, 2016Co-Authors: Guohua Wang, Chen Zang, Baoxian Zhang, Qixia Nie, Qiong Zhu, Gan Luo, Shuang WangAbstract:This study aimed to design a nanocarrier ophthalmic delivery system of Muscone, a poorly water-soluble drug. The Muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high Muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is <5 s. Compared with Muscone eye drops, Muscone nanogels showed longer retention time on the corneal surface using fluorescent labeling technology and produced a 3.4-fold increase in apparent permeability coefficients (Papp). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of Muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.
Abdelmottaleb Ben Lamine - One of the best experts on this subject based on the ideXlab platform.
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stereochemical study of mouse Muscone receptor mor215 1 and vibrational theory based on statistical physics formalism
Progress in Biophysics & Molecular Biology, 2018Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Abdelmottaleb Ben LamineAbstract:Abstract In the biosensor system, olfactory receptor sites could be activated by odorant molecules and then the biological interactions are converted into electrical signals by a signal transduction cascade that leads the toopening of ion channels, generating a current that leads into the cilia and depolarizes the membrane. The aim of this paper is to present a new investigation that allows determining the olfactory band using a monolayer adsorption with identical sites modeling which may also describe the static and the dynamic sensitivities through the expression of the olfactory response. Moreover, knowing the size of receptor site in olfactory sensory neurons provides valuable information about the relationship between molecular structure and biological activity. The determination of microreceptors and mesoreceptors is mostly carried out via physical adsorption and the radius is calculated using the Kelvin equation. The mean values of radius obtained from the maximum of the receptor size distributions peaks are 4 nm for l-Muscone and 6 nm for d-Muscone.
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olfactory response modeling of mouse Muscone receptor mor215 1 to binary Muscone enantiomers odor by statistical physics models
Journal of Molecular Liquids, 2016Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Abdelmottaleb Ben LamineAbstract:Abstract In this paper, an adsorption modeling has been presented to describe the interactions of a binary mixture of l-Muscone and d-Muscone with the mouse Muscone receptor MOR215-1. The formulation of the 2-dimensional monolayer models with identical and two types of sites for the perceived response of odor binary mixture odor are based on statistical physics and some theoretical hypothesis, in order to model pure and binary mixture dose-response curves. Thanks to the grand canonical ensemble of statistical physics, some pertinent physico-chemical parameters describing the adsorption process were introduced in the analytical model expressions. The results showed a high correlation of the 2-dimensional monolayer model using two types of sites with binary mixture of l-Muscone and d-Muscone response curve. In this model, six physico-chemical parameters derived from the fitting of the experimental data by a numerical simulation were discussed. Furthermore, these statistical physics models include physico-chemical parameters specific to the respective effects of each compound in the binary mixture, which may help to clarify the inhibitory effects that are often seen in l-Muscone and d-Muscone mixture through the determination of the involved new steric parameters. In addition, the calculation of the molar adsorption energies showed that the two Muscone enantiomers and their racemic were physisorbed onto cell surface neurons.
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modeling of Muscone enantiomers olfactory response by an adsorption process onto the mouse Muscone receptor mor215 1
Journal of Molecular Liquids, 2016Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Lotfi Sellaoui, Abdelmottaleb Ben LamineAbstract:Abstract The olfactory response curves of Muscone enantiomers on the mouse Muscone receptor MOR215-1 modeling by a statistical physics treatment led us to better understand the olfactory phenomenon. Our objective in this modeling is to select an adequate model that presents a significant correlation with the olfactory response curves. The application of the grand canonical ensemble in statistical thermodynamics introduces some physico-chemical parameters in the theoretical model which allows to attain an expression of the single olfactory response Rsin. Fitting results showed that the Muscone enantiomers ( l -Muscone and d -Muscone) followed an adsorption model with one monolayer onto identical sites. The calculation of the molar adsorption energy showed that the two Muscone enantiomers were physisorbed onto cell surface neurons. Then, the configurational entropy which gave an idea about order and disorder, was calculated according to the appropriate model.
Guohua Wang - One of the best experts on this subject based on the ideXlab platform.
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self assembled thermoresponsive nanogels prepared by reverse micelle positive micelle method for ophthalmic delivery of Muscone a poorly water soluble drug
Journal of Pharmaceutical Sciences, 2016Co-Authors: Guohua Wang, Chen Zang, Baoxian Zhang, Shuang WangAbstract:Abstract This study aimed to design a nanocarrier ophthalmic delivery system of Muscone, a poorly water-soluble drug. The Muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high Muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is P app ). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of Muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.
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self assembled thermoresponsive nanogels prepared by reverse micelle positive micelle method for ophthalmic delivery of Muscone a poorly water soluble drug
Journal of Pharmaceutical Sciences, 2016Co-Authors: Guohua Wang, Chen Zang, Baoxian Zhang, Qixia Nie, Qiong Zhu, Gan Luo, Shuang WangAbstract:This study aimed to design a nanocarrier ophthalmic delivery system of Muscone, a poorly water-soluble drug. The Muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high Muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is <5 s. Compared with Muscone eye drops, Muscone nanogels showed longer retention time on the corneal surface using fluorescent labeling technology and produced a 3.4-fold increase in apparent permeability coefficients (Papp). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of Muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.
Ismahene Ben Khemis - One of the best experts on this subject based on the ideXlab platform.
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stereochemical study of mouse Muscone receptor mor215 1 and vibrational theory based on statistical physics formalism
Progress in Biophysics & Molecular Biology, 2018Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Abdelmottaleb Ben LamineAbstract:Abstract In the biosensor system, olfactory receptor sites could be activated by odorant molecules and then the biological interactions are converted into electrical signals by a signal transduction cascade that leads the toopening of ion channels, generating a current that leads into the cilia and depolarizes the membrane. The aim of this paper is to present a new investigation that allows determining the olfactory band using a monolayer adsorption with identical sites modeling which may also describe the static and the dynamic sensitivities through the expression of the olfactory response. Moreover, knowing the size of receptor site in olfactory sensory neurons provides valuable information about the relationship between molecular structure and biological activity. The determination of microreceptors and mesoreceptors is mostly carried out via physical adsorption and the radius is calculated using the Kelvin equation. The mean values of radius obtained from the maximum of the receptor size distributions peaks are 4 nm for l-Muscone and 6 nm for d-Muscone.
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olfactory response modeling of mouse Muscone receptor mor215 1 to binary Muscone enantiomers odor by statistical physics models
Journal of Molecular Liquids, 2016Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Abdelmottaleb Ben LamineAbstract:Abstract In this paper, an adsorption modeling has been presented to describe the interactions of a binary mixture of l-Muscone and d-Muscone with the mouse Muscone receptor MOR215-1. The formulation of the 2-dimensional monolayer models with identical and two types of sites for the perceived response of odor binary mixture odor are based on statistical physics and some theoretical hypothesis, in order to model pure and binary mixture dose-response curves. Thanks to the grand canonical ensemble of statistical physics, some pertinent physico-chemical parameters describing the adsorption process were introduced in the analytical model expressions. The results showed a high correlation of the 2-dimensional monolayer model using two types of sites with binary mixture of l-Muscone and d-Muscone response curve. In this model, six physico-chemical parameters derived from the fitting of the experimental data by a numerical simulation were discussed. Furthermore, these statistical physics models include physico-chemical parameters specific to the respective effects of each compound in the binary mixture, which may help to clarify the inhibitory effects that are often seen in l-Muscone and d-Muscone mixture through the determination of the involved new steric parameters. In addition, the calculation of the molar adsorption energies showed that the two Muscone enantiomers and their racemic were physisorbed onto cell surface neurons.
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modeling of Muscone enantiomers olfactory response by an adsorption process onto the mouse Muscone receptor mor215 1
Journal of Molecular Liquids, 2016Co-Authors: Ismahene Ben Khemis, Nesrine Mechi, Lotfi Sellaoui, Abdelmottaleb Ben LamineAbstract:Abstract The olfactory response curves of Muscone enantiomers on the mouse Muscone receptor MOR215-1 modeling by a statistical physics treatment led us to better understand the olfactory phenomenon. Our objective in this modeling is to select an adequate model that presents a significant correlation with the olfactory response curves. The application of the grand canonical ensemble in statistical thermodynamics introduces some physico-chemical parameters in the theoretical model which allows to attain an expression of the single olfactory response Rsin. Fitting results showed that the Muscone enantiomers ( l -Muscone and d -Muscone) followed an adsorption model with one monolayer onto identical sites. The calculation of the molar adsorption energy showed that the two Muscone enantiomers were physisorbed onto cell surface neurons. Then, the configurational entropy which gave an idea about order and disorder, was calculated according to the appropriate model.
