Marco Mor

Summary

Affiliation: University of Parma
Country: Italy

Publications

  1. ncbi Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Italy
    J Pineal Res 36:95-102. 2004
  2. ncbi Antioxidant and cytoprotective activity of indole derivatives related to melatonin
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma
    Adv Exp Med Biol 527:567-75. 2003
  3. doi Synthesis and stability in biological media of 1H-imidazole-1-carboxylates of ROS203, an antagonist of the histamine H3 receptor
    Mirko Rivara
    Dipartimento Farmaceutico, Viale G P Usberti 27 A, I 43100 Parma
    Chem Biodivers 5:140-52. 2008
  4. ncbi Validation of a histamine H3 receptor model through structure-activity relationships for classical H3 antagonists
    Simone Lorenzi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma, Italy
    Bioorg Med Chem 13:5647-57. 2005
  5. pmc Structure-property relationships of a class of carbamate-based fatty acid amide hydrolase (FAAH) inhibitors: chemical and biological stability
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Viale G P Usberti 27A, Campus Universitario, 43100 Parma, Italy
    ChemMedChem 4:1495-504. 2009
  6. doi Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion
    Caterina Carmi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Vle GP Usberti 27 A, I 43124 Parma, Italy
    J Med Chem 53:2038-50. 2010
  7. doi Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain
    Fabrizio Bordi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43124 Parma, Italy
    Eur J Med Chem 48:214-30. 2012
  8. ncbi Application of 3D-QSAR in the rational design of receptor ligands and enzyme inhibitors
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle 27 A, I 43100 Parma
    Chem Biodivers 2:1438-51. 2005
  9. doi Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity
    Giovanni Morini
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43100 Parma, Italy
    Bioorg Med Chem 16:9911-24. 2008
  10. ncbi Imidazole H3-antagonists: relationship between structure and ex vivo binding to rat brain H3-receptors
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27A, I 43100 Parma, Italy
    Eur J Pharm Sci 23:89-98. 2004

Collaborators

Detail Information

Publications68

  1. ncbi Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Italy
    J Pineal Res 36:95-102. 2004
    ....
  2. ncbi Antioxidant and cytoprotective activity of indole derivatives related to melatonin
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma
    Adv Exp Med Biol 527:567-75. 2003
    ..This compound was selected as the lead compound for a further SAR study, devoted to the optimization of the cytoprotective effect and to the investigation on its mechanism...
  3. doi Synthesis and stability in biological media of 1H-imidazole-1-carboxylates of ROS203, an antagonist of the histamine H3 receptor
    Mirko Rivara
    Dipartimento Farmaceutico, Viale G P Usberti 27 A, I 43100 Parma
    Chem Biodivers 5:140-52. 2008
    ..However, the high rates of bioconversion in liver, as well as the chemical instability of 1h, suggest that further work is needed to optimize the enzymatic and chemical stability of these compounds...
  4. ncbi Validation of a histamine H3 receptor model through structure-activity relationships for classical H3 antagonists
    Simone Lorenzi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma, Italy
    Bioorg Med Chem 13:5647-57. 2005
    ....
  5. pmc Structure-property relationships of a class of carbamate-based fatty acid amide hydrolase (FAAH) inhibitors: chemical and biological stability
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Viale G P Usberti 27A, Campus Universitario, 43100 Parma, Italy
    ChemMedChem 4:1495-504. 2009
    ....
  6. doi Novel irreversible epidermal growth factor receptor inhibitors by chemical modulation of the cysteine-trap portion
    Caterina Carmi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Vle GP Usberti 27 A, I 43124 Parma, Italy
    J Med Chem 53:2038-50. 2010
    ....
  7. doi Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain
    Fabrizio Bordi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43124 Parma, Italy
    Eur J Med Chem 48:214-30. 2012
    ..Diastereoisomers with opposite chirality at the benzylic carbon showed limited or no stereoselectivity at both human and rat receptors...
  8. ncbi Application of 3D-QSAR in the rational design of receptor ligands and enzyme inhibitors
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle 27 A, I 43100 Parma
    Chem Biodivers 2:1438-51. 2005
    ..Some examples of the application of CoMFA and CoMSIA approaches to the SAR study and design of receptor or enzyme ligands is described, pointing the attention to the fields of melatonin receptor ligands and FAAH inhibitors...
  9. doi Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity
    Giovanni Morini
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43100 Parma, Italy
    Bioorg Med Chem 16:9911-24. 2008
    ..70; pK(B)=9.28). These compounds can be considered as rigid analogs of a recently reported class of dual-acting compounds and as a promising starting point for the design of new H(3)-antagonists with anti-cholinesterase activity...
  10. ncbi Imidazole H3-antagonists: relationship between structure and ex vivo binding to rat brain H3-receptors
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27A, I 43100 Parma, Italy
    Eur J Pharm Sci 23:89-98. 2004
    ..4) (apparent lipophilicity at pH 7.4) and DeltalogPoct-dce (a descriptor of H-bond donor capacity) allowed to model brain permeation of the majority of the compounds examined...
  11. doi Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors
    Federica Vacondio
    Dipartimento di Farmacia, Universita degli Studi di Parma, Parma, Italy
    Bioorg Med Chem Lett 23:5290-4. 2013
    ..Compounds 5-6 showed similar potency and duration of inhibition of EGFR autophosphorylation as the covalent inhibitor 2, while being devoid of reactive groups forming covalent bonds with protein thiols. ..
  12. doi N-(Anilinoethyl)amides: design and synthesis of metabolically stable, selective melatonin receptor ligands
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27A, Campus Universitario, 43124 Parma Italy, Fax 39 0521 905006
    ChemMedChem 4:1746-55. 2009
    ....
  13. ncbi Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists
    Gilberto Spadoni
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27A, Campus Universitario, 43100 Parma, Italy
    ChemMedChem 2:1741-9. 2007
    ..Docking experiments with an MT(2) receptor model suggested binding modes consistent with the observed SARs and with the lack of selectivity of the enantiomers of 5...
  14. pmc Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Viale GP Usberti 27 A, I 43124 Parma, Italy
    Eur J Med Chem 46:4466-73. 2011
    ..The SPRs here described may be applied at the pharmacokinetic optimization of other classes of carbamate FAAH inhibitors...
  15. ncbi Synthesis and biological evaluation of new non-imidazole H3-receptor antagonists of the 2-aminobenzimidazole series
    Mirko Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, Italy
    Bioorg Med Chem 14:1413-24. 2006
    ....
  16. ncbi Development and validation of a LC-MS method with electrospray ionization for the determination of the imidazole H3 antagonist ROS203 in rat plasma
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Viale G P Usberti 27 A, 43100 Parma, Italy
    J Pharm Biomed Anal 46:200-5. 2008
    ..The reported method can provide the necessary sensitivity, linearity, precision, accuracy and specificity to allow the determination of ROS203 in rat plasma samples to support further pharmacokinetic assays...
  17. doi 5-Benzylidene-hydantoins: synthesis and antiproliferative activity on A549 lung cancer cell line
    Valentina Zuliani
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43100 Parma, Italy
    Eur J Med Chem 44:3471-9. 2009
    ..Compound 7 and other synthesized 5-benzylidene hydantoin derivatives increased p53 levels, suggesting that the dual mechanism of action was a common feature shared by compound 7 and other member of the series...
  18. ncbi N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, Campus Universitario, 43100 Parma, Italy
    J Med Chem 50:6618-26. 2007
    ..The phenyl derivative 3g is an MT2-selective partial agonist, with MT2 binding affinity higher than melatonin, showing promising sleep-promoting and antianxiety properties in animal models...
  19. doi Synthesis and structure-activity relationships of amino acid conjugates of cholanic acid as antagonists of the EphA2 receptor
    Simonetta Russo
    Dipartimento di Farmacia, Universita degli Studi di Parma, Viale delle Scienze 27 A, Parma I 43124, Italy
    Molecules 18:13043-60. 2013
    ..These findings may help the design of novel EphA2 antagonists active on cancer cell lines. ..
  20. ncbi Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold
    Giovanni Morini
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43100 Parma, Italy
    Bioorg Med Chem Lett 16:4063-7. 2006
    ..47) at human H3 histamine receptor...
  21. doi Understanding the role of carbamate reactivity in fatty acid amide hydrolase inhibition by QM/MM mechanistic modelling
    Alessio Lodola
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parma, Italy
    Chem Commun (Camb) 47:2517-9. 2011
    ....
  22. ncbi Reassessing the melatonin pharmacophore--enantiomeric resolution, pharmacological activity, structure analysis, and molecular modeling of a constrained chiral melatonin analogue
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, 43100 Parma, Italy
    Bioorg Med Chem 14:3383-91. 2006
    ..Chiral enantioselective agonists reported in the literature were also included in the study...
  23. ncbi Synthesis, biological activity, QSAR and QSPR study of 2-aminobenzimidazole derivatives as potent H3-antagonists
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma, Italy
    Bioorg Med Chem 12:663-74. 2004
    ..Multiple regression analysis (MRA) showed an approximate parabolic dependence of pK(i) on log P, while an additional electronic effect of the substituents on benzimidazole tautomerism is suspected...
  24. pmc Quantum mechanics/molecular mechanics modeling of fatty acid amide hydrolase reactivation distinguishes substrate from irreversible covalent inhibitors
    Alessio Lodola
    Dipartimento di Farmacia, Universita degli Studi di Parma, I 43124 Parma, Italy
    J Med Chem 56:2500-12. 2013
    ..This is consistent with experimental data showing slowly reversible FAAH inhibition for the N-piperazinylurea inhibitor and irreversible inhibition for URB597...
  25. doi Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides
    Caterina Carmi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43124 Parma, Italy
    J Med Chem 55:2251-64. 2012
    ....
  26. pmc Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, viale G P Usberti 27 A Campus Universitario, I 43100 Parma, Italy
    J Med Chem 51:3487-98. 2008
    ..3 nM) and its 3'-carbamoylbiphenyl-3-yl ester 4z (URB880, IC50 = 0.63 nM), indicating that shape complementarity and hydrogen bonds are crucial to obtain highly potent inhibitors...
  27. doi Application of computational methods to the design of fatty acid amide hydrolase (FAAH) inhibitors based on a carbamic template structure
    Alessio Lodola
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, Parma, Italy
    Adv Protein Chem Struct Biol 85:1-26. 2011
    ..Latest advancements in the field are also reported...
  28. ncbi Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Italy
    J Med Chem 48:4049-60. 2005
    ..These results confirm the importance of the out-of-plane group in receptor binding and selectivity and provide a partial validation of the proposed G protein-coupled receptor model...
  29. doi Brain pharmacokinetics of non-imidazole biphenyl H3 receptor antagonists: a liquid chromatography/electrospray-mass spectrometry and ex vivo binding study in rats
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parma, Italy
    Chem Biodivers 9:1231-9. 2012
    ..plasma concentration ratios, if compared to 1. These structure´ú┐property relationships should be taken into account in the pharmacokinetic optimization of new series of H3 receptor antagonists...
  30. doi Application of a SCC-DFTB QM/MM approach to the investigation of the catalytic mechanism of fatty acid amide hydrolase
    Luigi Capoferri
    Dipartimento Farmaceutico, Universita degli Studi di Parma, viale G P Usberti 27 A Campus Universitario, 43124, Parma, Italy
    J Mol Model 17:2375-83. 2011
    ..All these findings indicate that the SCC-DFTB/CHARMM27 approach can be successfully applied to mechanistic investigations of FAAH-catalyzed reactions...
  31. ncbi Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Italy
    Expert Opin Ther Pat 20:1059-77. 2010
    ..Due to the multiple effects of this hormone, the design of new agents able to interact selectively with melatonin receptors has become an area of great interest during the last decade...
  32. doi Structure-based virtual screening of MT2 melatonin receptor: influence of template choice and structural refinement
    Daniele Pala
    Dipartimento di Farmacia, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43124 Parma, Italy
    J Chem Inf Model 53:821-35. 2013
    ..The top MT2 receptor model was able to identify 24 of 29 active ligands among the first 2% of the screened database. This work provides insights into the use of refined GPCR homology models for virtual screening...
  33. doi Chiral NMR discrimination of the diastereoisomeric salts of the H3-antagonist 2-[3-(1H-imidazol-4-ylmethyl)piperidin-1-yl]-1H-benzimidazole
    Mirko Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti, 27 a, I 43100 Parma, Italy
    Magn Reson Chem 47:515-8. 2009
    ..Chemical-shift differences (Delta delta) in NMR spectra strongly depend on solvent and stoichiometric ratio. The better observable differentiation occurred for the proton at the 2-position of the imidazole ring...
  34. ncbi Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, Campus Universitario, 43100 Parma, Italy
    Curr Top Med Chem 8:954-68. 2008
    ..A brief discussion on the therapeutic potential of this class of compounds is based on the clinical data available for the agonists ramelteon, agomelatine, beta-methyl-6-chloromelatonin (TIK-301) and VEC-162...
  35. doi Liquid chromatography-mass spectrometric method for determination of the non-imidazole H3-receptor antagonist UPR1056 in rat plasma
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parma, Italy
    J Sep Sci 34:1656-63. 2011
    ....
  36. ncbi Synthesis and three-dimensional quantitative structure-activity relationship analysis of H3 receptor antagonists containing a neutral heterocyclic polar group
    Silvia Rivara
    Universita degli Studi di Parma, Parma, Italy
    Drug Des Discov 18:65-79. 2003
    ..The 3D-QSAR models thus obtained showed that H(3) receptor affinity is modulated by the position and direction of the intermolecular interaction elicited by the polar group in the ligands...
  37. ncbi Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation
    Silvia Rivara
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, Italy
    J Med Chem 46:1429-39. 2003
    ..The reliability of our statistical models was further confirmed by the correct prediction of the pharmacological behavior of some N-substituted melatonin derivatives, which were prepared and tested on cloned receptor subtypes...
  38. doi Insights into the mechanism and inhibition of fatty acid amide hydrolase from quantum mechanics/molecular mechanics (QM/MM) modelling
    Alessio Lodola
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parma, Italy
    Biochem Soc Trans 37:363-7. 2009
    ..These are potentially crucial insights for designing new covalent inhibitors of this drug target...
  39. doi Qualitative structure-metabolism relationships in the hydrolysis of carbamates
    Federica Vacondio
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parma, Italy
    Drug Metab Rev 42:551-89. 2010
    ..This trend should prove useful in the design of carbamates as drugs or prodrugs...
  40. ncbi Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors
    Silvia Rivara
    Dipartimento di Farmacia, Universita degli Studi di Parma, Viale G P Usberti 27 A, I 43124 Parma, Italy
    J Med Chem 56:1247-61. 2013
    ..Two analogues of 17f, namely 18b and 19a, inhibit MAO-B with IC(50) of 68 and 48 nM, respectively, being 5-7-fold more potent than the prototypical MAO-B inhibitor deprenyl (IC(50) = 334 nM)...
  41. ncbi 5-benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity
    Caterina Carmi
    Dipartimento Farmaceutico, Universita degli Studi di Parma, V le G P Usberti 27 A, I 43100 Parma, Italy
    Bioorg Med Chem Lett 16:4021-5. 2006
    ..These compounds can therefore be regarded as examples of a new scaffold for tyrosine kinase inhibitors...
  42. doi Catalytic, asymmetric hypervinylogous Mukaiyama aldol reactions of extended furan-based silyl enolates
    Claudio Curti
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27A, I 43124 Parma, Italy
    Org Lett 13:4738-41. 2011
    ....
  43. ncbi Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma, Italy
    J Med Chem 47:4998-5008. 2004
    ..The structure-activity characterization reported here should help optimize the pharmacodynamic and pharmacokinetic properties of this class of compounds...
  44. pmc Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor
    Matteo Incerti
    Dipartimento di Farmacia, Universita degli Studi di Parma, Viale delle Scienze 27 A, I 43124 Parma, Italy
    J Med Chem 56:2936-47. 2013
    ..Compound 20 is among the most potent small-molecule antagonists of the EphA2 receptor...
  45. doi Pharmacological tools in endocannabinoid neurobiology
    Marco Mor
    Dipartimento Farmaceutico, Universita degli Studi di Parma, viale G P Usberti 27 A Campus Universitario, Parma, I 43100, Italy
    Curr Top Behav Neurosci 1:87-110. 2009
    ....
  46. ncbi pH-partition profiles of 4-(3-oxo-1,2-benzisothiazolin-2-yl)phenyl and phenoxyalkanoic acids
    Claudia Silva
    Dipartimento Farmaceutico, Universita degli Studi di Parma, Parco Area delle Scienze 27 A, I 43100 Parma, Italy
    Farmaco 58:989-93. 2003
    ..The 1,2-benzisothiazolin-3-one nucleus behaves as a lipophilic, moderately electron-withdrawing group...
  47. doi Complex product composition generates risks for generic substitution also with dosage forms for intravenous administration
    Alessandra Rossi
    Department of Pharmacy, University of Parma, Parco Area delle Scienze 27 A, 43124 Parma, Italy
    Int J Pharm 451:50-6. 2013
    ..The results obtained show that PCA can distinguish the differing origin of this biological drug...
  48. ncbi Synthesis, pharmacological evaluation, and structure-activity relationships of benzopyran derivatives with potent SERM activity
    Gabriele Amari
    Department of Medicinal Chemistry, Chiesi Farmaceutici s p a, Via Palermo 26 A, I 43100 Parma, Italy
    Bioorg Med Chem 12:3763-82. 2004
    ..This selectivity can be ascribed to differences in amino acid composition and side chain conformation in the region accommodating the 3-phenyl ring at human ER alpha and ER beta ligand-binding domain...
  49. ncbi Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors
    Giorgio Tarzia
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino Carlo Bo, Piazza del Rinascimento 6, Italy
    J Med Chem 46:2352-60. 2003
    ..URB524 (N-cyclohexylcarbamic acid biphenyl-3-yl ester, 9g) is the most potent compound of the series (IC(50) = 63 nM) and was therefore selected for further optimization...
  50. ncbi Synthesis and structure-activity relationships of a series of pyrrole cannabinoid receptor agonists
    Giorgio Tarzia
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino Carlo Bo, Piazza del Rinascimento 6, I 61029 Urbino, Italy
    Bioorg Med Chem 11:3965-73. 2003
    ....
  51. ncbi Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands
    Annalida Bedini
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino Carlo Bo, Piazza Rinascimento 6, 61029 Urbino, Italy
    J Med Chem 49:7393-403. 2006
    ..The MT(2) expected binding affinities of the new compounds were calculated by a previously developed 3D-QSAR CoMFA model, giving satisfactory predictions...
  52. ncbi The fatty-acid amide hydrolase inhibitor URB597 does not affect triacylglycerol hydrolysis in rat tissues
    Jason R Clapper
    Center for Drug Discovery, University of California, Irvine, CA 92697, USA
    Pharmacol Res 54:341-4. 2006
    ..The results indicate that URB597, while potent at inhibiting FAAH, does not affect TGH and TGL activities in rat tissues...
  53. ncbi Modulation of anxiety through blockade of anandamide hydrolysis
    Satish Kathuria
    Department of Pharmacology, University of California, Irvine, California, USA
    Nat Med 9:76-81. 2003
    ..Our results indicate that anandamide participates in the modulation of emotional states and point to fatty acid amide hydrolase inhibition as an innovative approach to anti-anxiety therapy...
  54. ncbi Synthesis, antioxidant activity and structure-activity relationships for a new series of 2-(N-acylaminoethyl)indoles with melatonin-like cytoprotective activity
    Gilberto Spadoni
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino Carlo Bo, Urbino, Italy
    J Pineal Res 40:259-69. 2006
    ....
  55. pmc URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices
    Alvin R King
    Department of Pharmacology, University of California, Irvine, Irvine, CA 92697, USA
    Chem Biol 14:1357-65. 2007
    ..Thus, URB602 may provide a useful tool by which to investigate the physiological roles of 2-AG and explore the potential interest of MGL as a therapeutic target...
  56. ncbi Strategies leading to MT2 selective melatonin receptor antagonists
    Gilberto Spadoni
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino, Piazza Rinascimento 6, I 61029 Urbino, Italy
    Adv Exp Med Biol 527:577-85. 2003
    ..This paper reviews our progress in developing subtype selective melatonin antagonists. Evidence is presented suggesting the structural features conferring MT2 selective antagonism...
  57. ncbi Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity
    Valeria Lucini
    Dipartimento di Farmacologia, Chemioterapia e Tossicologia Medica, Universita degli Studi di Milano, Via Vanvitelli 32, I 20129 Milano, Italy
    J Med Chem 47:4202-12. 2004
    ..The acetamide derivative 4b produced a noticeable reduction of GTPgammaS binding at MT2 receptor, thus being among the few inverse agonists described...
  58. ncbi Pharmacological characterization of hydrolysis-resistant analogs of oleoylethanolamide with potent anorexiant properties
    Giuseppe Astarita
    Department of Pharmacology, 360 MSRII, University of California, Irvine, CA 92697 4625, USA
    J Pharmacol Exp Ther 318:563-70. 2006
    ..These results suggest that the endogenous high-affinity PPAR-alpha agonist OEA may provide a scaffold for the discovery of novel orally active PPAR-alpha ligands...
  59. pmc Conformational effects in enzyme catalysis: reaction via a high energy conformation in fatty acid amide hydrolase
    Alessio Lodola
    Biophys J 92:L20-2. 2007
    ..They also show that approaches based simply on studying enzyme-substrate complexes can be misleading for understanding biochemical reactivity...
  60. ncbi Synthesis and structure-activity relationships of FAAH inhibitors: cyclohexylcarbamic acid biphenyl esters with chemical modulation at the proximal phenyl ring
    Giorgio Tarzia
    Istituto di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Urbino Carlo Bo, Piazza del Rinascimento 6, 61029 Urbino, Italy
    ChemMedChem 1:130-9. 2006
    ..Derivatives with small polar groups at the para position of the proximal phenyl ring were slightly better FAAH inhibitors than the parent compound URB524...
  61. ncbi The fatty acid amide hydrolase inhibitor URB597 (cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester) reduces neuropathic pain after oral administration in mice
    Roberto Russo
    Department of Experimental Pharmacology, University of Naples, Italy
    J Pharmacol Exp Ther 322:236-42. 2007
    ..The results provide new evidence for a role of the endocannabinoid system in pain modulation and reinforce the proposed role of FAAH as a target for analgesic drug development...
  62. ncbi Antidepressant-like activity of the fatty acid amide hydrolase inhibitor URB597 in a rat model of chronic mild stress
    Marco Bortolato
    Department of Pharmacology, University of California, Irvine, California 92697 4260, USA
    Biol Psychiatry 62:1103-10. 2007
    ....
  63. ncbi Selective inhibition of 2-AG hydrolysis enhances endocannabinoid signaling in hippocampus
    Judit K Makara
    Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, 8 Szigony u 43, Budapest, H 1083 Hungary
    Nat Neurosci 8:1139-41. 2005
    ..These results establish a role for 2-AG in synaptic plasticity and point to monoacylglycerol lipase as a possible drug target...
  64. ncbi An endocannabinoid mechanism for stress-induced analgesia
    Andrea G Hohmann
    Neuroscience and Behavior Program, Department of Psychology, The University of Georgia, Athens, Georgia 30602 3013, USA
    Nature 435:1108-12. 2005
    ..These studies also identify monoacylglycerol lipase as a previously unrecognized therapeutic target...
  65. ncbi Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitors
    Giovanni Valitutti
    J Mass Spectrom 42:1624-7. 2007
  66. ncbi Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597): effects on anandamide and oleoylethanolamide deactivation
    Darren Fegley
    Department of Pharmacology, University of California, Irvine CA 92697 4625, USA
    J Pharmacol Exp Ther 313:352-8. 2005
    ..The results also suggest that an enzyme distinct from FAAH catalyzes OEA hydrolysis in the duodenum, where this lipid substance acts as a local satiety factor...
  67. ncbi Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597)
    Daniele Piomelli
    Kadmus Pharmaceuticals, Inc Irvine, California 92697 4625, USA
    CNS Drug Rev 12:21-38. 2006
    ..The results suggest that KDS-4103 will offer a novel approach with a favorable therapeutic window for the treatment of anxiety, depression and pain...
  68. ncbi Tandem mass spectrometric data-FAAH inhibitory activity relationships of some carbamic acid O-aryl esters
    Elisa Basso
    CNR, Istituto di Scienze e Tecnologie Molecolari, Corso Stati Uniti 4, 35127 Padova, Italy
    J Mass Spectrom 39:1450-5. 2004
    ..797) with their FAAH-inhibitory activity. This indicates that the energetics of the C(O)--O bond cleavage may be relevant in explaining FAAH inhibition...