The Experts below are selected from a list of 258 Experts worldwide ranked by ideXlab platform
Philip G. Jessop - One of the best experts on this subject based on the ideXlab platform.
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Use of CO2-Triggered Switchable Surfactants for the Stabilization of Oil-in-Water Emulsions
Energy & Fuels, 2011Co-Authors: Chen Liang, Jitendra R. Harjani, Tobias Robert, Estrella Rogel, Donald L. Kuehne, Cesar Ovalles, Vasudevan Sampath, Philip G. JessopAbstract:Pipelining of heavy crudes can be facilitated by preparing oil-in-water (O/W) emulsions of the crude, but separation of the oil from the water after pipelining is problematic if conventional surfactants are used. Long-chain Acetamidines are CO2-triggered switchable surfactants, being surface-active when CO2 is present but not when CO2 is absent. Unfortunately, in the presence of CO2, they stabilize water-in-oil (W/O) emulsions of heavy crude rather than the desired O/W emulsions. However, in the absence of added CO2, several compounds (Na2CO3, three of the long-chain Acetamidines, and two other amidines) stabilize O/W emulsions. These low-viscosity emulsions can later be broken by the addition of CO2. The residual oil content in the recovered water is lowest if the compound used to stabilize the original emulsion was a long-chain Acetamidine.
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A synthesis of Acetamidines.
The Journal of organic chemistry, 2011Co-Authors: Jitendra R. Harjani, Chen Liang, Philip G. JessopAbstract:The condensation of primary amine with N,N-dimethylacetamide dimethyl acetal yields a mixture of Acetamidine and imidate ester. The product distribution in this reaction depends on the temperature, solvent, and structure of the primary amine. It is possible to suppress the formation of imidate ester by performing the reaction in the presence of excess dimethyl amine, yielding Acetamidine as the exclusive product. For Acetamidines that cannot be purified either by crystallization or distillation, this new method is necessary for the generation of pure Acetamidines in good yields.
Cristina Maccallini - One of the best experts on this subject based on the ideXlab platform.
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A novel prodrug of a nNOS inhibitor with improved pharmacokinetic potential.
ChemMedChem, 2020Co-Authors: Cristina Maccallini, Marialuigia Fantacuzzi, Lisa Marinelli, Patrick Indorf, Ivana Cacciatore, Bernd Clement, Antonio Di Stefano, Rosa AmorosoAbstract:Under different pathological conditions, aberrant induction of neuronal nitric oxide synthase (nNOS) generates overproduction of NO that can cause irreversible cell damage. The aim of this study was to develop an amidoxime prodrug of a potent nNOS inhibitor, the benzhydryl Acetamidine. We synthesized the benzhydryl acetamidoxime, which was evaluated in vitro to ascertain the potential NOS inhibitory activity, as well as conducting bioconversion into the parent Acetamidine. The prodrug was also profiled for in vitro physicochemical properties, by determining the lipophilicity, passive permeation through the human gastrointestinal tract and across the blood-brain barrier by PAMPA, and chemical, enzymatic, and plasma stability. The obtained data demonstrate that the amidoxime prodrug shows an improved pharmacokinetic profile with respect to the Acetamidine nNOS inhibitor, thus suggesting that it could be a promising lead compound to treat all those pathological conditions in which nNOS activity is dysregulated.
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Selective inhibition of inducible nitric oxide synthase by derivatives of Acetamidine.
Medicinal chemistry (Shariqah (United Arab Emirates)), 2012Co-Authors: Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Sara Franceschelli, Letizia Giampietro, Simona Masella, Maria Luisa Tricca, Rosa AmorosoAbstract:A new series of phenyl- and heteryl Acetamidines were synthesized and evaluated as inhibitors of nitric oxide synthases (NOS). While the N-substitution of the Acetamidine moiety with different heterocycles appears to completely destroy the activity, linking the phenyl core preserves it. Moreover, it was observed a strong dependence of the phenylAcetamidines potency of action from the length of the alkyl chain that connects the aromatic ring to the Acetamidine moiety.
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N-Substituted Acetamidines and 2-methylimidazole derivatives as selective inhibitors of neuronal nitric oxide synthase.
Bioorganic & medicinal chemistry letters, 2010Co-Authors: Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Sara Franceschelli, Letizia Giampietro, Simona Masella, Fabio Lannutti, Mario FelacoAbstract:Abstract A series of N-substituted Acetamidines and 2-methylimidazole derivatives structurally related to W1400 were synthesized and evaluated as Nitric Oxide Synthase (NOS) inhibitors. Analogs with sterically hindering isopropyl and phenyl substituents on the benzylic carbon connecting the aromatic core of W1400 to the Acetamidine nitrogen, showed good inhibitory potency for nNOS (IC 50 = 0.2 and 0.3 μM) and selectivity over eNOS (500 and 1166) and to a lesser extent over iNOS (50 and 100). A molecular modeling study allowed to shed light on the effects of the structural modifications on the selectivity of the designed inhibitors toward the different NOS isoforms.
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Synthesis, Biological Evaluation, and Docking Studies of N-Substituted Acetamidines as Selective Inhibitors of Inducible Nitric Oxide Synthase
Journal of medicinal chemistry, 2009Co-Authors: Cristina Maccallini, Antonia Patruno, Alessandra Ammazzalorso, Barbara De Filippis, Sara Franceschelli, Letizia Giampietro, Neva Bešker, Jamila Isabella Alì, Mirko Pesce, Marcella RealeAbstract:New Acetamidines structurally related to N-(3-(aminomethyl)benzyl)Acetamidine (1, W1400) were designed as inhibitors of inducible nitric oxide synthase (iNOS). Six compounds were found to be selective for iNOS over endothelial nitric oxide synthase (eNOS), and among them, the most active and selective compound was the N-benzylAcetamidine 2. A docking study was also performed to shed light on the effects of the structural modifications on the interaction of the designed inhibitors with the NOS.
Stephen J. Lee - One of the best experts on this subject based on the ideXlab platform.
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S‐2‐Naphthylmethyl Thioacetimidate Hydrobromide: A New Odorless Reagent for the Mild Synthesis of Substituted Acetamidines.
ChemInform, 2010Co-Authors: Barry G. Shearer, Jeffrey A. Oplinger, Stephen J. LeeAbstract:Abstract The development, synthesis and use of S-2-naphthylmethyl thioacetimidate hydrobromide 7 as a highly reactive reagent for the mild conversion of amines to substituted Acetamidines in a nonodorous process is described.
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S-2-Naphthylmethyl thioacetimidate hydrobromide: A new odorless reagent for the mild synthesis of substituted Acetamidines
Tetrahedron Letters, 1997Co-Authors: Barry G. Shearer, Jeffrey A. Oplinger, Stephen J. LeeAbstract:Abstract The development, synthesis and use of S-2-naphthylmethyl thioacetimidate hydrobromide 7 as a highly reactive reagent for the mild conversion of amines to substituted Acetamidines in a nonodorous process is described.
Chen Liang - One of the best experts on this subject based on the ideXlab platform.
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Use of CO2-Triggered Switchable Surfactants for the Stabilization of Oil-in-Water Emulsions
Energy & Fuels, 2011Co-Authors: Chen Liang, Jitendra R. Harjani, Tobias Robert, Estrella Rogel, Donald L. Kuehne, Cesar Ovalles, Vasudevan Sampath, Philip G. JessopAbstract:Pipelining of heavy crudes can be facilitated by preparing oil-in-water (O/W) emulsions of the crude, but separation of the oil from the water after pipelining is problematic if conventional surfactants are used. Long-chain Acetamidines are CO2-triggered switchable surfactants, being surface-active when CO2 is present but not when CO2 is absent. Unfortunately, in the presence of CO2, they stabilize water-in-oil (W/O) emulsions of heavy crude rather than the desired O/W emulsions. However, in the absence of added CO2, several compounds (Na2CO3, three of the long-chain Acetamidines, and two other amidines) stabilize O/W emulsions. These low-viscosity emulsions can later be broken by the addition of CO2. The residual oil content in the recovered water is lowest if the compound used to stabilize the original emulsion was a long-chain Acetamidine.
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A synthesis of Acetamidines.
The Journal of organic chemistry, 2011Co-Authors: Jitendra R. Harjani, Chen Liang, Philip G. JessopAbstract:The condensation of primary amine with N,N-dimethylacetamide dimethyl acetal yields a mixture of Acetamidine and imidate ester. The product distribution in this reaction depends on the temperature, solvent, and structure of the primary amine. It is possible to suppress the formation of imidate ester by performing the reaction in the presence of excess dimethyl amine, yielding Acetamidine as the exclusive product. For Acetamidines that cannot be purified either by crystallization or distillation, this new method is necessary for the generation of pure Acetamidines in good yields.
A. Grob - One of the best experts on this subject based on the ideXlab platform.
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N,N′‐Bis(benzyloxycarbonyl)Acetamidine, a Versatile Reagent for the Conversion of Amines and Alcohols to Acetamidines.
ChemInform, 2010Co-Authors: J. Eustache, A. GrobAbstract:Abstract N,N′-Bis(benzyloxycarbonyl)Acetamidine is the prototype of a new class of versatile reagents for the conversion of amines and alcohols to substituted amidines. The preparation of 1 and its potential uses are described.
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n n bis benzyloxycarbonyl Acetamidine a versatile reagent for the conversion of amines and alcohols to Acetamidines
ChemInform, 1995Co-Authors: J. Eustache, A. GrobAbstract:Abstract N,N′-Bis(benzyloxycarbonyl)Acetamidine is the prototype of a new class of versatile reagents for the conversion of amines and alcohols to substituted amidines. The preparation of 1 and its potential uses are described.
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N,N′-Bis(benzyloxycarbonyl)Acetamidine, a versatile reagent for the conversion of amines and alcohols to Acetamidines
Tetrahedron Letters, 1995Co-Authors: J. Eustache, A. GrobAbstract:Abstract N,N′-Bis(benzyloxycarbonyl)Acetamidine is the prototype of a new class of versatile reagents for the conversion of amines and alcohols to substituted amidines. The preparation of 1 and its potential uses are described.
