The Experts below are selected from a list of 1887 Experts worldwide ranked by ideXlab platform
Gerard Aime Pinna - One of the best experts on this subject based on the ideXlab platform.
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3 2 bis 4 fluorophenyl methoxy ethyl 6 substituted 3 6 diazabicyclo 3 1 1 heptanes as novel potent dopamine uptake inhibitors
Bioorganic & Medicinal Chemistry, 2007Co-Authors: Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Gabriele Murineddu, Christian Dessi, Luca Pani, Gerard Aime PinnaAbstract:Abstract A series of analogues 2a–i related to 3-{2-[bis-(4-fluorophenyl)methoxy]ethyl}-8-(1H-indol-2-ylmethyl)-3,8-diazabicyclo[3.2.1]octane (1) in which the 3,8-diazabicyclo[3.2.1]octane core was replaced by 3,6-diazabicyclo[3.1.1]heptane ring system has been synthesized and evaluated for their ability to inhibit DA reuptake into striatal nerve endings (synaptosomes). Biological data showed that compound 2a, the closest analogue of lead 1, possessed an increased reuptake inhibition activity over 1 (2a, Ki = 5.5 nM). Replacement of the indole ring with bioisosteric aromatic rings—benzothiophene (2b), benzofurane (2c), or indene (2d)—resulted, with the exception of 2d, in a double digit nanomolar activity. Changing the indenyl moiety of 2d with simplified aryl groups led to compounds 2e–h which displayed a similar or slightly decreased activity with respect to the ground term. Naphthalene Derivative (2i) demonstrated a weaker activity than aromatic analogues.
Giovanni Loriga - One of the best experts on this subject based on the ideXlab platform.
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3 2 bis 4 fluorophenyl methoxy ethyl 6 substituted 3 6 diazabicyclo 3 1 1 heptanes as novel potent dopamine uptake inhibitors
Bioorganic & Medicinal Chemistry, 2007Co-Authors: Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Gabriele Murineddu, Christian Dessi, Luca Pani, Gerard Aime PinnaAbstract:Abstract A series of analogues 2a–i related to 3-{2-[bis-(4-fluorophenyl)methoxy]ethyl}-8-(1H-indol-2-ylmethyl)-3,8-diazabicyclo[3.2.1]octane (1) in which the 3,8-diazabicyclo[3.2.1]octane core was replaced by 3,6-diazabicyclo[3.1.1]heptane ring system has been synthesized and evaluated for their ability to inhibit DA reuptake into striatal nerve endings (synaptosomes). Biological data showed that compound 2a, the closest analogue of lead 1, possessed an increased reuptake inhibition activity over 1 (2a, Ki = 5.5 nM). Replacement of the indole ring with bioisosteric aromatic rings—benzothiophene (2b), benzofurane (2c), or indene (2d)—resulted, with the exception of 2d, in a double digit nanomolar activity. Changing the indenyl moiety of 2d with simplified aryl groups led to compounds 2e–h which displayed a similar or slightly decreased activity with respect to the ground term. Naphthalene Derivative (2i) demonstrated a weaker activity than aromatic analogues.
Jing Zhang - One of the best experts on this subject based on the ideXlab platform.
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a novel two photon fluorescent probe for the selective detection of hydrogen peroxide based on a Naphthalene Derivative
Analytical Methods, 2017Co-Authors: Jing Zhang, Liyi Zhou, Xiaoyan Zhu, Hongwen LiuAbstract:In this study, we report a novel two-photon fluorescent probe for monitoring hydrogen peroxide. Probe 1 consists of a Naphthalene backbone and a boric acid ester which was used as a H2O2 reporter. The reaction of probe 1 with H2O2 triggers the cleavage of a boronate-based protecting group, and as a result, restores the fluorescence of compound 2. The probe can be applied to the quantification of hydrogen peroxide with a linear range from 1.0 × 10−6 to 2.5 × 10−4 mol L−1. The detection limit of probe 1 toward H2O2 was estimated to be 0.7 μM. Furthermore, probe 1 was found to have a much higher selectivity for H2O2 than other reactive oxygen species and successfully applied to cell imaging of hydrogen peroxide using two-photon microscopy in living cells. The superior properties of the probe made it highly promising for use in chemical and biological applications.
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ratiometric two photon fluorescent probe for in vivo hydrogen polysulfides detection and imaging during lipopolysaccharide induced acute organs injury
Analytical Chemistry, 2016Co-Authors: Jing Zhang, Xiaobing Zhang, Xiaoyan Zhu, Hongwen Liu, Lili Feng, Xia Yin, Weihong TanAbstract:Acute organ injury observed during sepsis, caused by an uncontrolled release of inflammatory mediators, such as lipopolysaccharide (LPS), is quite fatal. The development of efficient methods for early diagnosis of sepsis and LPS-induced acute organ injury in living systems is of great biomedical importance. In living systems, cystathionine γ-lyase (CSE) can be overexpressed due to LPS, and H2Sn can be formed by CSE-mediated cysteine metabolism. Thus, acute organ injury during sepsis may be correlated with H2Sn levels, making accurate detection of H2Sn in living systems of great physiological and pathological significance. In this work, our previously reported fluorescent platform was employed to design and synthesize a FRET-based ratiometric two-photon (TP) fluorescent probe TPR-S, producing a large emission shift in the presence of H2Sn. In this work, a Naphthalene Derivative two-photon fluorophore was chosen as the energy donor; a rhodol Derivative fluorophore served as the acceptor. The 2-fluoro-5-nitr...
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molecular engineering of a tbet based two photon fluorescent probe for ratiometric imaging of living cells and tissues
Journal of the American Chemical Society, 2014Co-Authors: Liyi Zhou, Qianqian Wang, Xiaobing Zhang, Yifan Lv, Yongxiang Wu, Yuan Wu, Jing ZhangAbstract:In contrast to one-photon microscopy, two-photon probe-based fluorescent imaging can provide improved three-dimensional spatial localization and increased imaging depth. Consequently, it has become one of the most attractive techniques for studying biological events in living cells and tissues. However, the quantitation of these probes is primarily based on single-emission intensity change, which tends to be affected by a variety of environmental factors. Ratiometric probes, on the other hand, can eliminate these interferences by the built-in correction of the dual emission bands, resulting in a more favorable system for imaging living cells and tissues. Herein, for the first time, we adopted a through-bond energy transfer (TBET) strategy to design and synthesize a small molecular ratiometric two-photon fluorescent probe for imaging living cells and tissues in real time. Specifically, a two-photon fluorophore (D-π-A-structured Naphthalene Derivative) and a rhodamine B fluorophore are directly connected by...
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high sensitivity Naphthalene based two photon fluorescent probe suitable for direct bioimaging of h2s in living cells
Analytical Chemistry, 2013Co-Authors: Xuxiang Wang, Xiaobing Zhang, Jing Zhang, Shuangyan Huan, Danqing Lu, Guoli Shen, Ruqin YuAbstract:H2S is the third endogenously generated gaseous signaling compound and has also been known to involve a variety of physiological processes. To better understand its physiological and pathological functions, efficient methods for monitoring of H2S in living systems are desired. Although quite a few one photon fluorescence probes have been reported for H2S, two-photon (TP) probes are more favorable for intracellular imaging. In this work, by employing a donor-π-acceptor-structured Naphthalene Derivative as the two-photon fluorophore and an azide group as the recognition unit, we reported a new two-photon bioimaging probe 6-(benzo[d]thiazol-2′-yl)-2-azidoNaphthalene (NHS1) for H2S with improved sensitivity. The probe shows very low background fluorescence in the absence of H2S. In the presence of H2S, however, a significant enhancement for both one photon and TP excited fluorescence were observed, resulting in a high sensitivity to H2S in aqueous solutions with a detection limit of 20 nM observed, much lower...
Ilaria Manca - One of the best experts on this subject based on the ideXlab platform.
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3 2 bis 4 fluorophenyl methoxy ethyl 6 substituted 3 6 diazabicyclo 3 1 1 heptanes as novel potent dopamine uptake inhibitors
Bioorganic & Medicinal Chemistry, 2007Co-Authors: Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Gabriele Murineddu, Christian Dessi, Luca Pani, Gerard Aime PinnaAbstract:Abstract A series of analogues 2a–i related to 3-{2-[bis-(4-fluorophenyl)methoxy]ethyl}-8-(1H-indol-2-ylmethyl)-3,8-diazabicyclo[3.2.1]octane (1) in which the 3,8-diazabicyclo[3.2.1]octane core was replaced by 3,6-diazabicyclo[3.1.1]heptane ring system has been synthesized and evaluated for their ability to inhibit DA reuptake into striatal nerve endings (synaptosomes). Biological data showed that compound 2a, the closest analogue of lead 1, possessed an increased reuptake inhibition activity over 1 (2a, Ki = 5.5 nM). Replacement of the indole ring with bioisosteric aromatic rings—benzothiophene (2b), benzofurane (2c), or indene (2d)—resulted, with the exception of 2d, in a double digit nanomolar activity. Changing the indenyl moiety of 2d with simplified aryl groups led to compounds 2e–h which displayed a similar or slightly decreased activity with respect to the ground term. Naphthalene Derivative (2i) demonstrated a weaker activity than aromatic analogues.
Christian Dessi - One of the best experts on this subject based on the ideXlab platform.
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3 2 bis 4 fluorophenyl methoxy ethyl 6 substituted 3 6 diazabicyclo 3 1 1 heptanes as novel potent dopamine uptake inhibitors
Bioorganic & Medicinal Chemistry, 2007Co-Authors: Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Gabriele Murineddu, Christian Dessi, Luca Pani, Gerard Aime PinnaAbstract:Abstract A series of analogues 2a–i related to 3-{2-[bis-(4-fluorophenyl)methoxy]ethyl}-8-(1H-indol-2-ylmethyl)-3,8-diazabicyclo[3.2.1]octane (1) in which the 3,8-diazabicyclo[3.2.1]octane core was replaced by 3,6-diazabicyclo[3.1.1]heptane ring system has been synthesized and evaluated for their ability to inhibit DA reuptake into striatal nerve endings (synaptosomes). Biological data showed that compound 2a, the closest analogue of lead 1, possessed an increased reuptake inhibition activity over 1 (2a, Ki = 5.5 nM). Replacement of the indole ring with bioisosteric aromatic rings—benzothiophene (2b), benzofurane (2c), or indene (2d)—resulted, with the exception of 2d, in a double digit nanomolar activity. Changing the indenyl moiety of 2d with simplified aryl groups led to compounds 2e–h which displayed a similar or slightly decreased activity with respect to the ground term. Naphthalene Derivative (2i) demonstrated a weaker activity than aromatic analogues.
