Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 145

1.

Potent, Metabolically Stable 2-Alkyl-8-(2H-1,2,3-triazol-2-yl)-9H-adenines as Adenosine A2A Receptor Ligands.

Pace S, Brogin G, Stasi MA, Riccioni T, Borsini F, Capocasa F, Manera F, Tallarico C, Grossi P, Vacondio F, Bassi M, Bartoccini F, Lucarini S, Piersanti G, Tarzia G, Cabri W, Minetti P.

ChemMedChem. 2015 Jul;10(7):1149-52. doi: 10.1002/cmdc.201500113. Epub 2015 May 7.

PMID:
25951302
2.

A Potent Systemically Active N-Acylethanolamine Acid Amidase Inhibitor that Suppresses Inflammation and Human Macrophage Activation.

Ribeiro A, Pontis S, Mengatto L, Armirotti A, Chiurchiù V, Capurro V, Fiasella A, Nuzzi A, Romeo E, Moreno-Sanz G, Maccarrone M, Reggiani A, Tarzia G, Mor M, Bertozzi F, Bandiera T, Piomelli D.

ACS Chem Biol. 2015 Aug 21;10(8):1838-46. doi: 10.1021/acschembio.5b00114. Epub 2015 Apr 15.

3.

Selective melatonin MT2 receptor ligands relieve neuropathic pain through modulation of brainstem descending antinociceptive pathways.

Lopez-Canul M, Palazzo E, Dominguez-Lopez S, Luongo L, Lacoste B, Comai S, Angeloni D, Fraschini F, Boccella S, Spadoni G, Bedini A, Tarzia G, Maione S, Granados-Soto V, Gobbi G.

Pain. 2015 Feb;156(2):305-17. doi: 10.1097/01.j.pain.0000460311.71572.5f.

PMID:
25599452
4.

Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain.

Moreno-Sanz G, Barrera B, Armirotti A, Bertozzi SM, Scarpelli R, Bandiera T, Prieto JG, Duranti A, Tarzia G, Merino G, Piomelli D.

Pharmacol Res. 2014 Sep;87:87-93. doi: 10.1016/j.phrs.2014.06.004. Epub 2014 Jun 30.

5.

3-Aminoazetidin-2-one derivatives as N-acylethanolamine acid amidase (NAAA) inhibitors suitable for systemic administration.

Fiasella A, Nuzzi A, Summa M, Armirotti A, Tarozzo G, Tarzia G, Mor M, Bertozzi F, Bandiera T, Piomelli D.

ChemMedChem. 2014 Jul;9(7):1602-14. doi: 10.1002/cmdc.201300546. Epub 2014 May 14.

6.

Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.

Spadoni G, Bedini A, Bartolucci S, Pala D, Mor M, Riccioni T, Borsini F, Cabri W, Celona D, Marzi M, Tarzia G, Rivara S, Minetti P.

Eur J Med Chem. 2014 Jun 10;80:8-35. doi: 10.1016/j.ejmech.2014.04.034. Epub 2014 Apr 13.

PMID:
24763360
7.

Melatonin, selective and non-selective MT1/MT2 receptors agonists: differential effects on the 24-h vigilance states.

Ochoa-Sanchez R, Comai S, Spadoni G, Bedini A, Tarzia G, Gobbi G.

Neurosci Lett. 2014 Feb 21;561:156-61. doi: 10.1016/j.neulet.2013.12.069. Epub 2014 Jan 7.

PMID:
24406151
8.

Synthesis and structure-activity relationship (SAR) of 2-methyl-4-oxo-3-oxetanylcarbamic acid esters, a class of potent N-acylethanolamine acid amidase (NAAA) inhibitors.

Ponzano S, Bertozzi F, Mengatto L, Dionisi M, Armirotti A, Romeo E, Berteotti A, Fiorelli C, Tarozzo G, Reggiani A, Duranti A, Tarzia G, Mor M, Cavalli A, Piomelli D, Bandiera T.

J Med Chem. 2013 Sep 12;56(17):6917-34. doi: 10.1021/jm400739u. Epub 2013 Aug 30.

9.

Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.

Moreno-Sanz G, Duranti A, Melzig L, Fiorelli C, Ruda GF, Colombano G, Mestichelli P, Sanchini S, Tontini A, Mor M, Bandiera T, Scarpelli R, Tarzia G, Piomelli D.

J Med Chem. 2013 Jul 25;56(14):5917-30. doi: 10.1021/jm4007017. Epub 2013 Jul 3.

10.

Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.

Piersanti G, Bartoccini F, Lucarini S, Cabri W, Stasi MA, Riccioni T, Borsini F, Tarzia G, Minetti P.

J Med Chem. 2013 Jul 11;56(13):5456-63. doi: 10.1021/jm400491x. Epub 2013 Jun 24.

PMID:
23789814
11.

Quantum mechanics/molecular mechanics modeling of fatty acid amide hydrolase reactivation distinguishes substrate from irreversible covalent inhibitors.

Lodola A, Capoferri L, Rivara S, Tarzia G, Piomelli D, Mulholland A, Mor M.

J Med Chem. 2013 Mar 28;56(6):2500-12. doi: 10.1021/jm301867x. Epub 2013 Mar 7.

12.

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

Rivara S, Piersanti G, Bartoccini F, Diamantini G, Pala D, Riccioni T, Stasi MA, Cabri W, Borsini F, Mor M, Tarzia G, Minetti P.

J Med Chem. 2013 Feb 14;56(3):1247-61. doi: 10.1021/jm301686s. Epub 2013 Jan 16.

PMID:
23281824
13.

Editorial: premature publishing and over-fragmentation.

Tarzia G.

ChemMedChem. 2013 Jan;8(1):6-7. doi: 10.1002/cmdc.201200494. No abstract available.

PMID:
23281336
14.

Antinociceptive effects of the N-acylethanolamine acid amidase inhibitor ARN077 in rodent pain models.

Sasso O, Moreno-Sanz G, Martucci C, Realini N, Dionisi M, Mengatto L, Duranti A, Tarozzo G, Tarzia G, Mor M, Bertorelli R, Reggiani A, Piomelli D.

Pain. 2013 Mar;154(3):350-60. doi: 10.1016/j.pain.2012.10.018. Epub 2012 Nov 2.

15.

Divergent synthesis of novel 9-deazaxanthine derivatives via late-stage cross-coupling reactions.

Bartoccini F, Piersanti G, Mor M, Tarzia G, Minetti P, Cabri W.

Org Biomol Chem. 2012 Nov 28;10(44):8860-7. doi: 10.1039/c2ob26516h.

PMID:
23047760
16.

MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides.

Rivara S, Pala D, Lodola A, Mor M, Lucini V, Dugnani S, Scaglione F, Bedini A, Lucarini S, Tarzia G, Spadoni G.

ChemMedChem. 2012 Nov;7(11):1954-64. doi: 10.1002/cmdc.201200303. Epub 2012 Aug 27.

PMID:
22927210
17.

Anxiolytic effects of the melatonin MT(2) receptor partial agonist UCM765: comparison with melatonin and diazepam.

Ochoa-Sanchez R, Rainer Q, Comai S, Spadoni G, Bedini A, Rivara S, Fraschini F, Mor M, Tarzia G, Gobbi G.

Prog Neuropsychopharmacol Biol Psychiatry. 2012 Dec 3;39(2):318-25. doi: 10.1016/j.pnpbp.2012.07.003. Epub 2012 Jul 10.

PMID:
22789661
18.

β-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine.

Armirotti A, Romeo E, Ponzano S, Mengatto L, Dionisi M, Karacsonyi C, Bertozzi F, Garau G, Tarozzo G, Reggiani A, Bandiera T, Tarzia G, Mor M, Piomelli D.

ACS Med Chem Lett. 2012 Apr 6;3(5):422-6. doi: 10.1021/ml300056y. eCollection 2012 May 10.

19.

N-(2-oxo-3-oxetanyl)carbamic acid esters as N-acylethanolamine acid amidase inhibitors: synthesis and structure-activity and structure-property relationships.

Duranti A, Tontini A, Antonietti F, Vacondio F, Fioni A, Silva C, Lodola A, Rivara S, Solorzano C, Piomelli D, Tarzia G, Mor M.

J Med Chem. 2012 May 24;55(10):4824-36. doi: 10.1021/jm300349j. Epub 2012 May 10.

20.

Promotion of non-rapid eye movement sleep and activation of reticular thalamic neurons by a novel MT2 melatonin receptor ligand.

Ochoa-Sanchez R, Comai S, Lacoste B, Bambico FR, Dominguez-Lopez S, Spadoni G, Rivara S, Bedini A, Angeloni D, Fraschini F, Mor M, Tarzia G, Descarries L, Gobbi G.

J Neurosci. 2011 Dec 14;31(50):18439-52. doi: 10.1523/JNEUROSCI.2676-11.2011.

21.

Toward the definition of stereochemical requirements for MT2-selective antagonists and partial agonists by studying 4-phenyl-2-propionamidotetralin derivatives.

Bedini A, Lucarini S, Spadoni G, Tarzia G, Scaglione F, Dugnani S, Pannacci M, Lucini V, Carmi C, Pala D, Rivara S, Mor M.

J Med Chem. 2011 Dec 22;54(24):8362-72. doi: 10.1021/jm200790v. Epub 2011 Nov 18.

PMID:
22047556
22.

Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.

Vacondio F, Silva C, Lodola A, Carmi C, Rivara S, Duranti A, Tontini A, Sanchini S, Clapper JR, Piomelli D, Tarzia G, Mor M.

Eur J Med Chem. 2011 Sep;46(9):4466-73. doi: 10.1016/j.ejmech.2011.07.021. Epub 2011 Jul 21.

23.

Bivalent ligand approach on N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide: synthesis, binding affinity and intrinsic activity for MT(1) and MT(2) melatonin receptors.

Spadoni G, Bedini A, Orlando P, Lucarini S, Tarzia G, Mor M, Rivara S, Lucini V, Pannacci M, Scaglione F.

Bioorg Med Chem. 2011 Aug 15;19(16):4910-6. doi: 10.1016/j.bmc.2011.06.063. Epub 2011 Jun 28.

PMID:
21775151
24.

ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors.

Riccioni T, Bordi F, Minetti P, Spadoni G, Yun HM, Im BH, Tarzia G, Rhim H, Borsini F.

Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14. doi: 10.1016/j.ejphar.2011.04.028. Epub 2011 Apr 28.

PMID:
21549693
25.

Understanding the role of carbamate reactivity in fatty acid amide hydrolase inhibition by QM/MM mechanistic modelling.

Lodola A, Capoferri L, Rivara S, Chudyk E, Sirirak J, Dyguda-Kazimierowicz E, Andrzej Sokalski W, Mileni M, Tarzia G, Piomelli D, Mor M, Mulholland AJ.

Chem Commun (Camb). 2011 Mar 7;47(9):2517-9. doi: 10.1039/c0cc04937a. Epub 2011 Jan 14.

26.

Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism.

Clapper JR, Moreno-Sanz G, Russo R, Guijarro A, Vacondio F, Duranti A, Tontini A, Sanchini S, Sciolino NR, Spradley JM, Hohmann AG, Calignano A, Mor M, Tarzia G, Piomelli D.

Nat Neurosci. 2010 Oct;13(10):1265-70. doi: 10.1038/nn.2632. Epub 2010 Sep 19.

27.

"Hot spots" in medicinal chemistry.

Metternich R, Tarzia G.

ChemMedChem. 2010 Aug 2;5(8):1159-62. doi: 10.1002/cmdc.201000266. No abstract available.

PMID:
20669174
28.

Synthesis and structure-activity relationships of N-(2-oxo-3-oxetanyl)amides as N-acylethanolamine-hydrolyzing acid amidase inhibitors.

Solorzano C, Antonietti F, Duranti A, Tontini A, Rivara S, Lodola A, Vacondio F, Tarzia G, Piomelli D, Mor M.

J Med Chem. 2010 Aug 12;53(15):5770-81. doi: 10.1021/jm100582w.

29.

Direct B-alkyl Suzuki-Miyaura cross-coupling of 2-halopurines. Practical synthesis of ST1535, a potent adenosine A2A receptor antagonist.

Bartoccini F, Cabri W, Celona D, Minetti P, Piersanti G, Tarzia G.

J Org Chem. 2010 Aug 6;75(15):5398-401. doi: 10.1021/jo101027h.

PMID:
20597521
30.

Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists.

Mor M, Rivara S, Pala D, Bedini A, Spadoni G, Tarzia G.

Expert Opin Ther Pat. 2010 Aug;20(8):1059-77. doi: 10.1517/13543776.2010.496455. Review.

PMID:
20533893
31.

Selective N-acylethanolamine-hydrolyzing acid amidase inhibition reveals a key role for endogenous palmitoylethanolamide in inflammation.

Solorzano C, Zhu C, Battista N, Astarita G, Lodola A, Rivara S, Mor M, Russo R, Maccarrone M, Antonietti F, Duranti A, Tontini A, Cuzzocrea S, Tarzia G, Piomelli D.

Proc Natl Acad Sci U S A. 2009 Dec 8;106(49):20966-71. doi: 10.1073/pnas.0907417106. Epub 2009 Nov 19.

32.

N-(Anilinoethyl)amides: design and synthesis of metabolically stable, selective melatonin receptor ligands.

Rivara S, Vacondio F, Fioni A, Silva C, Carmi C, Mor M, Lucini V, Pannacci M, Caronno A, Scaglione F, Gobbi G, Spadoni G, Bedini A, Orlando P, Lucarini S, Tarzia G.

ChemMedChem. 2009 Oct;4(10):1746-55. doi: 10.1002/cmdc.200900240.

PMID:
19728346
33.

A second generation of carbamate-based fatty acid amide hydrolase inhibitors with improved activity in vivo.

Clapper JR, Vacondio F, King AR, Duranti A, Tontini A, Silva C, Sanchini S, Tarzia G, Mor M, Piomelli D.

ChemMedChem. 2009 Sep;4(9):1505-13. doi: 10.1002/cmdc.200900210.

34.

Structure-property relationships of a class of carbamate-based fatty acid amide hydrolase (FAAH) inhibitors: chemical and biological stability.

Vacondio F, Silva C, Lodola A, Fioni A, Rivara S, Duranti A, Tontini A, Sanchini S, Clapper JR, Piomelli D, Mor M, Tarzia G.

ChemMedChem. 2009 Sep;4(9):1495-504. doi: 10.1002/cmdc.200900120.

35.

Rapid and transient stimulation of intracellular reactive oxygen species by melatonin in normal and tumor leukocytes.

Radogna F, Paternoster L, De Nicola M, Cerella C, Ammendola S, Bedini A, Tarzia G, Aquilano K, Ciriolo M, Ghibelli L.

Toxicol Appl Pharmacol. 2009 Aug 15;239(1):37-45. doi: 10.1016/j.taap.2009.05.012. Epub 2009 May 19.

PMID:
19463840
36.

Endocannabinoids in the treatment of mood disorders: evidence from animal models.

Bambico FR, Duranti A, Tontini A, Tarzia G, Gobbi G.

Curr Pharm Des. 2009;15(14):1623-46. Review.

PMID:
19442178
37.

Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice.

LoVerme J, Duranti A, Tontini A, Spadoni G, Mor M, Rivara S, Stella N, Xu C, Tarzia G, Piomelli D.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):639-43. doi: 10.1016/j.bmcl.2008.12.059. Epub 2008 Dec 24.

38.

The collisional behavior of ESI-generated protonated molecules of some carbamate FAAH inhibitors isosteres and its relationships with biological activity.

Valitutti G, Duranti A, Mor M, Piersanti G, Piomelli D, Rivara S, Tontini A, Tarzia G, Traldi P.

J Mass Spectrom. 2009 Apr;44(4):561-5. doi: 10.1002/jms.1524. No abstract available. Erratum in: J Mass Spectrom. 2011 Aug;46(8):847.

39.

Medicinal chemistry: defining itself.

Metternich R, Tarzia G.

ChemMedChem. 2008 Aug;3(8):1147-9. doi: 10.1002/cmdc.200800116. No abstract available.

PMID:
18693287
40.

Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders.

Rivara S, Mor M, Bedini A, Spadoni G, Tarzia G.

Curr Top Med Chem. 2008;8(11):954-68. Review.

PMID:
18673165
41.

Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.

Mor M, Lodola A, Rivara S, Vacondio F, Duranti A, Tontini A, Sanchini S, Piersanti G, Clapper JR, King AR, Tarzia G, Piomelli D.

J Med Chem. 2008 Jun 26;51(12):3487-98. doi: 10.1021/jm701631z. Epub 2008 May 29. Erratum in: J Med Chem. 2009 Jan 8;52(1):224.

42.

URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.

King AR, Duranti A, Tontini A, Rivara S, Rosengarth A, Clapper JR, Astarita G, Geaga JA, Luecke H, Mor M, Tarzia G, Piomelli D.

Chem Biol. 2007 Dec;14(12):1357-65.

43.

Identification of productive inhibitor binding orientation in fatty acid amide hydrolase (FAAH) by QM/MM mechanistic modelling.

Lodola A, Mor M, Rivara S, Christov C, Tarzia G, Piomelli D, Mulholland AJ.

Chem Commun (Camb). 2008 Jan 14;(2):214-6. Epub 2007 Oct 19.

PMID:
18092091
44.

Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitors.

Valitutti G, Duranti A, Lodola A, Mor M, Piersanti G, Piomelli D, Rivara S, Tontini A, Tarzia G, Traldi P.

J Mass Spectrom. 2007 Dec;42(12):1624-7. No abstract available.

45.

N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.

Rivara S, Lodola A, Mor M, Bedini A, Spadoni G, Lucini V, Pannacci M, Fraschini F, Scaglione F, Sanchez RO, Gobbi G, Tarzia G.

J Med Chem. 2007 Dec 27;50(26):6618-26. Epub 2007 Dec 6.

PMID:
18052314
46.

Synthesis of benzo[1,2-d;3,4-d']diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A2A receptor antagonists.

Piersanti G, Giorgi L, Bartoccini F, Tarzia G, Minetti P, Gallo G, Giorgi F, Castorina M, Ghirardi O, Carminati P.

Org Biomol Chem. 2007 Aug 21;5(16):2567-71.

PMID:
18019530
47.

Identification of a bioactive impurity in a commercial sample of 6-methyl-2-p-tolylaminobenzo[d][1,3]oxazin-4-one (URB754).

Tarzia G, Antonietti F, Duranti A, Tontini A, Mor M, Rivara S, Traldi P, Astarita G, King A, Clapper JR, Piomelli D.

Ann Chim. 2007 Sep;97(9):887-94.

48.

Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists.

Spadoni G, Bedini A, Diamantini G, Tarzia G, Rivara S, Lorenzi S, Lodola A, Mor M, Lucini V, Pannacci M, Caronno A, Fraschini F.

ChemMedChem. 2007 Dec;2(12):1741-9.

PMID:
17907131
49.

Melatonin antagonizes apoptosis via receptor interaction in U937 monocytic cells.

Radogna F, Paternoster L, Albertini MC, Cerella C, Accorsi A, Bucchini A, Spadoni G, Diamantini G, Tarzia G, De Nicola M, D'Alessio M, Ghibelli L.

J Pineal Res. 2007 Sep;43(2):154-62.

PMID:
17645693
50.

Antidepressant-like activity of the fatty acid amide hydrolase inhibitor URB597 in a rat model of chronic mild stress.

Bortolato M, Mangieri RA, Fu J, Kim JH, Arguello O, Duranti A, Tontini A, Mor M, Tarzia G, Piomelli D.

Biol Psychiatry. 2007 Nov 15;62(10):1103-10. Epub 2007 May 23.

Supplemental Content

Loading ...
Support Center