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Acid Amide

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Acid Amide – Free Register to Access Experts & Abstracts

John M Keith – One of the best experts on this subject based on the ideXlab platform.

Sandy J Wilson – One of the best experts on this subject based on the ideXlab platform.

  • Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
    Bioorganic & medicinal chemistry letters, 2014
    Co-Authors: John M Keith, Brian Scott, Mark Seierstad, Michael Webb, Mark J Karbarz, Sandy J Wilson, William M. Jones, Joan Pierce, James A. Palmer, Lin Luo
    Abstract:

    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.

  • Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
    Bioorganic & Medicinal Chemistry Letters, 2014
    Co-Authors: John M Keith, Brian Scott, Mark Seierstad, Michael Webb, Mark J Karbarz, William M. Jones, Joan Pierce, James A. Palmer, Sandy J Wilson
    Abstract:

    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.

  • thiadiazolopiperazinyl ureas as inhibitors of fatty Acid Amide hydrolase
    Bioorganic & Medicinal Chemistry Letters, 2008
    Co-Authors: John M Keith, Richard Apodaca, Wei Xiao, Mark Seierstad, Pattabiraman Kanaka, Michael Webb, Mark J Karbarz, Sean Brown, Sandy J Wilson, Brian Scott
    Abstract:

    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.

Brian Scott – One of the best experts on this subject based on the ideXlab platform.

  • Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
    Bioorganic & medicinal chemistry letters, 2014
    Co-Authors: John M Keith, Brian Scott, Mark Seierstad, Michael Webb, Mark J Karbarz, Sandy J Wilson, William M. Jones, Joan Pierce, James A. Palmer, Lin Luo
    Abstract:

    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.

  • Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty Acid Amide hydrolase.
    Bioorganic & Medicinal Chemistry Letters, 2014
    Co-Authors: John M Keith, Brian Scott, Mark Seierstad, Michael Webb, Mark J Karbarz, William M. Jones, Joan Pierce, James A. Palmer, Sandy J Wilson
    Abstract:

    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.

  • thiadiazolopiperazinyl ureas as inhibitors of fatty Acid Amide hydrolase
    Bioorganic & Medicinal Chemistry Letters, 2008
    Co-Authors: John M Keith, Richard Apodaca, Wei Xiao, Mark Seierstad, Pattabiraman Kanaka, Michael Webb, Mark J Karbarz, Sean Brown, Sandy J Wilson, Brian Scott
    Abstract:

    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.

  • Acid···Amide Supramolecular Synthon in Cocrystals: From Spectroscopic Detection to Property Engineering
    Journal of the American Chemical Society, 2018
    Co-Authors: Subhankar Saha, Gautam R Desiraju
    Abstract:

    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…

  • Acid Amide supramolecular synthon in cocrystals from spectroscopic detection to property engineering
    Journal of the American Chemical Society, 2018
    Co-Authors: Subhankar Saha, Gautam R Desiraju
    Abstract:

    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…