The Experts below are selected from a list of 312 Experts worldwide ranked by ideXlab platform
John M Keith - One of the best experts on this subject based on the ideXlab platform.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & medicinal chemistry letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Sandy J Wilson, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Lin LuoAbstract:A series of mechanism based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty Acid ethanolAmides [FAAs: anandAmide (AEA), oleoyl ethanolAmide (OEA) and palmitoyl ethanolAmide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Sandy J WilsonAbstract:Abstract A series of mechanism-based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.
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disruption of fatty Acid Amide hydrolase activity prevents the effects of chronic stress on anxiety and amygdalar microstructure
Molecular Psychiatry, 2013Co-Authors: Benjamin F Cravatt, Cecilia J. Hillard, John M Keith, Matthew N Hill, Shobha Anil Kumar, Sarah B Filipski, Moriah Iverson, Kara L Stuhr, Sumantra ChattarjiAbstract:Disruption of fatty Acid Amide hydrolase activity prevents the effects of chronic stress on anxiety and amygdalar microstructure
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thiadiazolopiperazinyl ureas as inhibitors of fatty Acid Amide hydrolase
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: John M Keith, Richard Apodaca, Wei Xiao, Mark Seierstad, Pattabiraman Kanaka, Michael Webb, Mark J Karbarz, Sean Brown, Sandy J Wilson, Brian ScottAbstract:A series of thiadiazolopiperazinyl aryl urea fatty Acid Amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
Sandy J Wilson - One of the best experts on this subject based on the ideXlab platform.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & medicinal chemistry letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Sandy J Wilson, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Lin LuoAbstract:A series of mechanism based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty Acid ethanolAmides [FAAs: anandAmide (AEA), oleoyl ethanolAmide (OEA) and palmitoyl ethanolAmide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Sandy J WilsonAbstract:Abstract A series of mechanism-based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.
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thiadiazolopiperazinyl ureas as inhibitors of fatty Acid Amide hydrolase
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: John M Keith, Richard Apodaca, Wei Xiao, Mark Seierstad, Pattabiraman Kanaka, Michael Webb, Mark J Karbarz, Sean Brown, Sandy J Wilson, Brian ScottAbstract:A series of thiadiazolopiperazinyl aryl urea fatty Acid Amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
Benjamin F Cravatt - One of the best experts on this subject based on the ideXlab platform.
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effects of fatty Acid Amide hydrolase faah inhibitors on working memory in rats
Psychopharmacology, 2016Co-Authors: Leigh V Panlilio, Benjamin F Cravatt, Alexandros Makriyannis, Daniele Piomelli, Eric B Thorndike, Spyros P Nikas, Shakiru O Alapafuja, Tiziano Bandiera, Steven R Goldberg, Zuzana JustinovaAbstract:Rationale Manipulations of the endocannabinoid system could potentially produce therapeutic effects with minimal risk of adverse cannabis-like side effects. Inhibitors of fatty Acid Amide hydrolase (FAAH) increase endogenous levels of the cannabinoid-receptor agonist, anandAmide, and show promise for treating a wide range of disorders. However, their effects on learning and memory have not been fully characterized.
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disruption of fatty Acid Amide hydrolase activity prevents the effects of chronic stress on anxiety and amygdalar microstructure
Molecular Psychiatry, 2013Co-Authors: Benjamin F Cravatt, Cecilia J. Hillard, John M Keith, Matthew N Hill, Shobha Anil Kumar, Sarah B Filipski, Moriah Iverson, Kara L Stuhr, Sumantra ChattarjiAbstract:Disruption of fatty Acid Amide hydrolase activity prevents the effects of chronic stress on anxiety and amygdalar microstructure
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Biochanin A, a naturally occurring inhibitor of fatty Acid Amide hydrolase.
British journal of pharmacology, 2010Co-Authors: Lina Thors, Roger G Pertwee, Benjamin F Cravatt, Michele K Mckinney, James J. Burston, Benedict J. Alter, Ruth A. Ross, Robert W. Gereau, Jenny L. Wiley, Christopher J. FowlerAbstract:BACKGROUND AND PURPOSE: Inhibitors of fatty Acid Amide hydrolase (FAAH), the enzyme responsible for the metabolism of the endogenous cannabinoid (CB) receptor ligand anandAmide (AEA), are effective ...
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Biochanin A acts as a peripheral inhibitor of fatty Acid Amide hydrolase
2009Co-Authors: Lina Thors, Roger G Pertwee, Benjamin F Cravatt, Michele K Mckinney, James J. Burston, Benedict J. Alter, Ruth A. Ross, Jenny L. Wiley, Robert W Gereau Th, Christopher J. FowlerAbstract:Inhibitors of fatty Acid Amide hydrolase (FAAH), the enzyme primarily responsible for the metabolism of the endogenous cannabinoid (CB) receptor ligand anandAmide, are effective in animal models of ...
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evaluation of fatty Acid Amide hydrolase inhibition in murine models of emotionality
Psychopharmacology, 2007Co-Authors: Pattipati S Naidu, Billy R. Martin, Benjamin F Cravatt, S A Varvel, Aron H LichtmanAbstract:Rationale Manipulations of the endocannabinoid/fatty Acid Amide hydrolase (FAAH) signaling systems result in conflicting and paradoxical effects in rodent models of emotional reactivity.
Brian Scott - One of the best experts on this subject based on the ideXlab platform.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & medicinal chemistry letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Sandy J Wilson, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Lin LuoAbstract:A series of mechanism based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty Acid ethanolAmides [FAAs: anandAmide (AEA), oleoyl ethanolAmide (OEA) and palmitoyl ethanolAmide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: John M Keith, Mark Seierstad, Michael Webb, Mark J Karbarz, Brian Scott, William M. Jones, Joan Pierce, James A. Palmer, Sandy J WilsonAbstract:Abstract A series of mechanism-based heteroaryl urea fatty Acid Amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.
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thiadiazolopiperazinyl ureas as inhibitors of fatty Acid Amide hydrolase
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: John M Keith, Richard Apodaca, Wei Xiao, Mark Seierstad, Pattabiraman Kanaka, Michael Webb, Mark J Karbarz, Sean Brown, Sandy J Wilson, Brian ScottAbstract:A series of thiadiazolopiperazinyl aryl urea fatty Acid Amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
Gautam R Desiraju - One of the best experts on this subject based on the ideXlab platform.
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Acid···Amide Supramolecular Synthon in Cocrystals: From Spectroscopic Detection to Property Engineering
Journal of the American Chemical Society, 2018Co-Authors: Subhankar Saha, Gautam R DesirajuAbstract:The Acid···Amide dimer heterosynthon in cocrystals of aromatic Acids and primary Amides is identified by marker peaks in the IR spectra that are characteristic of individual N–H···O and O–H···O interactions and also of the extended synthon. The O–H···O hydrogen bond is crucial to heterodimer formation in contrast to the N–H···O bond. A combinatorial study, tuning the chemical nature of Acid and Amide functionalities, leads to 22 cocrystals out of 36 crystallization attempts. Four quadrants I–IV are defined based on Acidity and basicity of the Acid and Amide components. The strong Acid–strong base combination in quadrant I favors the planar Acid···Amide heterodimer in its eight cocrystals. Quadrant IV with its weak Acid–weak base combination is the least favored for the planar heterosynthon and synthon diversity is observed in the eight cocrystals obtained. The strong–weak and weak–strong combinations in quadrants II and III are expectedly ambivalent. This exercise highlights the effect of molecular featur...
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Acid Amide supramolecular synthon in cocrystals from spectroscopic detection to property engineering
Journal of the American Chemical Society, 2018Co-Authors: Subhankar Saha, Gautam R DesirajuAbstract:The Acid···Amide dimer heterosynthon in cocrystals of aromatic Acids and primary Amides is identified by marker peaks in the IR spectra that are characteristic of individual N–H···O and O–H···O interactions and also of the extended synthon. The O–H···O hydrogen bond is crucial to heterodimer formation in contrast to the N–H···O bond. A combinatorial study, tuning the chemical nature of Acid and Amide functionalities, leads to 22 cocrystals out of 36 crystallization attempts. Four quadrants I–IV are defined based on Acidity and basicity of the Acid and Amide components. The strong Acid–strong base combination in quadrant I favors the planar Acid···Amide heterodimer in its eight cocrystals. Quadrant IV with its weak Acid–weak base combination is the least favored for the planar heterosynthon and synthon diversity is observed in the eight cocrystals obtained. The strong–weak and weak–strong combinations in quadrants II and III are expectedly ambivalent. This exercise highlights the effect of molecular featur...
