The Experts below are selected from a list of 534 Experts worldwide ranked by ideXlab platform
Sergio Tanganelli - One of the best experts on this subject based on the ideXlab platform.
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the vigilance promoting drug modafinil modulates serotonin transmission in the rat prefrontal cortex and dorsal raphe nucleus possible relevance for its postulated antidepressant activity
Mini-reviews in Medicinal Chemistry, 2013Co-Authors: Luca Ferraro, Tiziana Antonelli, Sarah Beggiato, Maria Cristina Tomasini, Kjell Fuxe, Sergio TanganelliAbstract:Modafinil, (RS)-2-(diphenylmethylsulfinyl)Acetamide Derivative (Modiodal, Provigil), is a vigilance-promoting agent which reduces sleep episodes by improving wakefulness. It is approved by the USA FDA for narcolepsy, shiftwork sleep disorder and obstructive sleep apnoea with residual excessive sleepiness despite optimal use of continuous positive airway pressure. Unlike classical psychostimulants such as amphetamine and amphetamine-like compounds, the awaking effect of modafinil is not associated with a disturbance of nighttime sleep, tolerance, and sensitization. Its precise mechanism of action is still unclear. In animal studies, modafinil and its analogues have been shown to modify dopaminergic, noradrenergic, glutamatergic, GABAergic, serotoninergic, orexinergic, and histaminergic pathways. Besides the approved use in sleep disorders, modafinil has been investigated for the treatment of fatigue, impaired cognition and some symptoms in a number of other disorders. In particular, clinical studies seem to indicate that the drug could be particularly successful in the treatment of depression and its use in major depressive and bipolar disorders, has been suggested. However, the molecular mechanisms underlying this possible effect are still unknown. The present review firstly summarizes the structure-activity relationship studies and the mechanism of action of modafinil and its related compounds. Then, it focuses on data demonstrating that modafinil interacts with serotonin neuronal activity in rat frontal cortex and dorsal raphe nucleus, two brain areas linked together and involved in depression. Preclinical and clinical evidence of a positive interaction between modafinil and classical antidepressant drugs, is also summarized.
Hidetoshi Tokuyama - One of the best experts on this subject based on the ideXlab platform.
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total syntheses of leuconoxine leuconodine b and melodinine e by oxidative cyclic aminal formation and diastereoselective ring closing metathesis
Organic Letters, 2014Co-Authors: Atsushi Umehara, Hirofumi Ueda, Hidetoshi TokuyamaAbstract:Total syntheses of leuconodine B, melodinine E, and leuconoxine were accomplished via a divergent route. The [5.5.6.6]diazafenestrane skeleton was constructed from an indole-3-Acetamide Derivative via DMDO oxidation to hydroxylindolenine, TMSOTf/2,6-lutidine mediated cyclic aminal formation, and diastereoseletive ring-closing metathesis of a triene Derivative.
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Total Syntheses of Leuconoxine, Leuconodine B, and Melodinine E by Oxidative Cyclic Aminal Formation and Diastereoselective Ring-Closing Metathesis
2014Co-Authors: Atsushi Umehara, Hirofumi Ueda, Hidetoshi TokuyamaAbstract:Total syntheses of leuconodine B, melodinine E, and leuconoxine were accomplished via a divergent route. The [5.5.6.6]diazafenestrane skeleton was constructed from an indole-3-Acetamide Derivative via DMDO oxidation to hydroxylindolenine, TMSOTf/2,6-lutidine mediated cyclic aminal formation, and diastereoseletive ring-closing metathesis of a triene Derivative
Mary J Garson - One of the best experts on this subject based on the ideXlab platform.
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absolute configuration and conformational study of psammaplysins a and b from the balinese marine sponge aplysinella strongylata
Journal of Natural Products, 2015Co-Authors: Attila Mandi, Wayan I Mudianta, Tibor Kurtan, Mary J GarsonAbstract:The absolute configuration of psammaplysin A (1) has been assigned as (6R,7R) using experimental and calculated electronic circular dichroism (ECD) data and NMR analysis of MPA esters prepared from the Acetamide Derivative of 1. Detailed conformational analyses of a truncated model compound of 1 with an in vacuo method and with the PCM solvent model for MeOH have identified the major conformers and factors governing the ECD spectrum of 1. The correlation of the ECD data with the stereochemistry of 1 allows configurational assignment of related psammaplysin analogues on the basis of their ECD spectra.
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Absolute Configuration and Conformational Study of Psammaplysins A and B from the Balinese Marine Sponge Aplysinella strongylata
2015Co-Authors: Attila Mándi, Wayan I Mudianta, Tibor Kurtán, Mary J GarsonAbstract:The absolute configuration of psammaplysin A (1) has been assigned as (6R,7R) using experimental and calculated electronic circular dichroism (ECD) data and NMR analysis of MPA esters prepared from the Acetamide Derivative of 1. Detailed conformational analyses of a truncated model compound of 1 with an in vacuo method and with the PCM solvent model for MeOH have identified the major conformers and factors governing the ECD spectrum of 1. The correlation of the ECD data with the stereochemistry of 1 allows configurational assignment of related psammaplysin analogues on the basis of their ECD spectra
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antifungal alkyl amino alcohols from the tropical marine sponge haliclona n sp
Journal of Natural Products, 2001Co-Authors: Richard J Clark, Mary J Garson, John N A HooperAbstract:Three new amino alcohols presumably deriving from L-alanine were isolated from the tropical marine sponge Haliclona n. sp. and characterized by 2D NMR, while a fourth amino alcohol was characterized as an Acetamide Derivative. Relative stereochemistry was deduced from the NMR characteristics of oxazolidinone Derivatives and absolute stereochemistry secured by preparation and analysis of an MPA ester. The amino alcohol fraction from Haliclona n. sp, acts as an antifungal agent and inhibits the development of larvae of the ascidian Herdmania curvata.
Luca Ferraro - One of the best experts on this subject based on the ideXlab platform.
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the vigilance promoting drug modafinil modulates serotonin transmission in the rat prefrontal cortex and dorsal raphe nucleus possible relevance for its postulated antidepressant activity
Mini-reviews in Medicinal Chemistry, 2013Co-Authors: Luca Ferraro, Tiziana Antonelli, Sarah Beggiato, Maria Cristina Tomasini, Kjell Fuxe, Sergio TanganelliAbstract:Modafinil, (RS)-2-(diphenylmethylsulfinyl)Acetamide Derivative (Modiodal, Provigil), is a vigilance-promoting agent which reduces sleep episodes by improving wakefulness. It is approved by the USA FDA for narcolepsy, shiftwork sleep disorder and obstructive sleep apnoea with residual excessive sleepiness despite optimal use of continuous positive airway pressure. Unlike classical psychostimulants such as amphetamine and amphetamine-like compounds, the awaking effect of modafinil is not associated with a disturbance of nighttime sleep, tolerance, and sensitization. Its precise mechanism of action is still unclear. In animal studies, modafinil and its analogues have been shown to modify dopaminergic, noradrenergic, glutamatergic, GABAergic, serotoninergic, orexinergic, and histaminergic pathways. Besides the approved use in sleep disorders, modafinil has been investigated for the treatment of fatigue, impaired cognition and some symptoms in a number of other disorders. In particular, clinical studies seem to indicate that the drug could be particularly successful in the treatment of depression and its use in major depressive and bipolar disorders, has been suggested. However, the molecular mechanisms underlying this possible effect are still unknown. The present review firstly summarizes the structure-activity relationship studies and the mechanism of action of modafinil and its related compounds. Then, it focuses on data demonstrating that modafinil interacts with serotonin neuronal activity in rat frontal cortex and dorsal raphe nucleus, two brain areas linked together and involved in depression. Preclinical and clinical evidence of a positive interaction between modafinil and classical antidepressant drugs, is also summarized.
Atsushi Umehara - One of the best experts on this subject based on the ideXlab platform.
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total syntheses of leuconoxine leuconodine b and melodinine e by oxidative cyclic aminal formation and diastereoselective ring closing metathesis
Organic Letters, 2014Co-Authors: Atsushi Umehara, Hirofumi Ueda, Hidetoshi TokuyamaAbstract:Total syntheses of leuconodine B, melodinine E, and leuconoxine were accomplished via a divergent route. The [5.5.6.6]diazafenestrane skeleton was constructed from an indole-3-Acetamide Derivative via DMDO oxidation to hydroxylindolenine, TMSOTf/2,6-lutidine mediated cyclic aminal formation, and diastereoseletive ring-closing metathesis of a triene Derivative.
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Total Syntheses of Leuconoxine, Leuconodine B, and Melodinine E by Oxidative Cyclic Aminal Formation and Diastereoselective Ring-Closing Metathesis
2014Co-Authors: Atsushi Umehara, Hirofumi Ueda, Hidetoshi TokuyamaAbstract:Total syntheses of leuconodine B, melodinine E, and leuconoxine were accomplished via a divergent route. The [5.5.6.6]diazafenestrane skeleton was constructed from an indole-3-Acetamide Derivative via DMDO oxidation to hydroxylindolenine, TMSOTf/2,6-lutidine mediated cyclic aminal formation, and diastereoseletive ring-closing metathesis of a triene Derivative
