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philippe.diaz

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Name: Philippe Diaz

Title: Research Associate Professor

Email: philippe.diaz@umontana.edu

Phone: 406-243-4362

Office: SB 479

Lab Phone: 406-243-4098

Lab: SB 152

Background

After completing his undergraduate studies in chemistry at the University of Nice (France) in 1990, Philippe Diaz earned a degree in engineering from the school of engineering in Marseille, France. Following, he carried out his graduate studies at the University Paul Cezanne in Marseille with Professor Lucien Stella and Dr. Charpentier, earning his Ph.D in organic chemistry in 1997. In the same year, he began his professional career in industry at Galderma R&D, France, where he progressed from team manager in medicinal chemistry, to head of Parallel chemistry department, and finally, to project monitor in research. In 2002, he earned his “Habilitation à diriger des recherches” from the Université de Montpellier 2, Montpellier, France. In 2006, Philippe joined M.D. Anderson Cancer Center as a Sr. Research scientist in the department of Anesthesiology and Pain Medicine. Philippe came to The University of Montana in 2009 to serve as manager of the Core Laboratory for Neuromolecular Production and was promoted to Research Associate Professor in 2010.

 

Research Statement

Neuropathic pain is a chronic condition of which the mechanism of action is still poorly understood. Neuropathic pain is triggered off by conditions such as diabetes, AIDS, postherpetic neuralgia, degenerative spinal disease, chemotherapy, radiotherapy, complex regional pain syndrome, phantom limb pain, trigeminal neuralgia, and multiple sclerosis. Treatments for neuropathic pain vary from antidepressant to anticonvulsant but are effective on fewer than 30% of patients.

Recently, however, the Cannabinoid receptor CB2 has emerged as a promising target for the treatment of neuropathic pain. CB2 is expressed mainly on immune tissues, and activation of CB2 does not cause psychotropic side effects. CB2 receptor stimulation suppresses glial cell activation and neuroinflammation. On the other hand, CB2 blockade has been shown to modulate immune cell mobility and to decrease inflammation in vivo and in vitro. We are currently designing and synthesizing novel compounds interacting with Cannabinoid receptors. We are studying whether these agents acting through CB2 receptors activation or blockade can modulate neuroinflammation and can be used as a novel treatment of neuropathic pain.

Recent findings suggest that in spinal cord glutamatergic neurons are involved in the pain signal in neuropathic pain. Glutamatergic activation promotes inflammation through MAPK phosphorylation. Our laboratory is exploring involvement of Glutamate/Glutamine cycle in the development of neuropathic pain. We are currently interested in the design and synthesis of modulators for Glutamate/Glutamine cycle as a potential target for the treatment of neuropathic pain.

Other ongoing projects involve design of innovative formulation for lipophilic drugs, such as nanoparticle-based drug delivery systems or innovative topical formulation.

 

Publications

Synthesis of New Quinolinequinone Derivatives and Preliminary Exploration of their Cytotoxic Properties. Keyari C.; Kearns A.; Duncan N.; Eickholt E.; Abbott G.; Beall H.; Diaz PJ.Med.Chem. 2013, 56(10):3806-3819DOI: 10.1021/jm301689xPMID:23574193

In vivo efficacy of enabling formulations based on hydroxypropyl-β-cyclodextrinsmicellar preparation and liposomes for the lipophilic cannabinoid CB2 agonist, MDA7Astruc-Diaz F.; McDaniel SW.; Xu JJ.; Parola S.; Brown DL.; Naguib M.; Diaz P. Journal of Pharmaceutical Sciences. 2013, 102(2):352-64. PMID:23192786

Prevention of Paclitaxel-Induced Neuropathy Through Activation of the Central Cannabinoid Type 2 Receptor System. Naguib M.; Xu J.J.; Diaz P.; Brown D.L.; Cogdell D.; Bie B.; Hu J.; Craig S.; Hittelman W.N. Anesthesia & Analgesia2012, 114(5), 1104-1120. PMID:22392969

Functional characterization and analgesic effects of mixed cannabinoid receptor/T-type channel ligands. You H.; Gadotti V.M.; Petrov R.R.; Zamponi G.W.; Diaz PMolecular Pain2011, 7:89. PMID:22093952

Neuroinflammation, Alzheimer’s Disease-Associated Pathology, and Down-Regulation of the Prion-Related Protein in Air Pollution Exposed Children and Young Adults. Calderón-Garcidueñas L.; Kavanaugh M.; Block M.; D'Angiulli A.; Delgado-Chávez R.; Torres-Jardón R.; González-Maciel A.; Reynoso-Robles R.; Osnaya N.; Villarreal-Calderon R.; Guo R.; Hua Z.; Zhu H.; Perry G.; Diaz PJ. Alzheimers Dis2011, 28 (1), 93-107.PMID:21955814

Suzuki–Miyaura cross-coupling of benzylic bromides under microwave conditions. McDaniel S. W.; Keyari C.M.; Rider K.C.; Natale N.R.; Diaz PTetrahedron Lett. 2011, 52, 5656-5658. PMID:21966033

Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells. Petrov R.R.; Ferrini M.E.; Jaffar Z.; Thompson C.M.; Roberts K.; Diaz PBioorg. Med. ChemLett. 2011, 21, 5859-5862. PMID:21855337

Pharmacological Characterization of a Novel Cannabinoid LigandMDA19, for Treatment of Neuropathic Pain. Xu J.; Diaz P.Astruc-Diaz F.; Craig S.; Munoz E.; and Naguib M. Anesthesia & Analgesia2010, 111 (1), 99-109.PMID:20522703

2,3-dihydro-1-benzofuran derivatives as a Novel Series of Potent Selective Cannabinoid Receptor 2 Agonists: Design, Synthesis, and Binding Mode Prediction. Philippe Diaz, Sharangdhar S. PhatakJijun Xu, Frank R. Fronczek, Fanny Astruc-Diaz, Claudio N. Cavasotto, Mohamed NaguibChemMedChem. 2009, 4, 1615-1629. Featured on cover page of issue.

6-Methoxy-N-alkyl Isatin Acylhydrazone Derivatives as a Novel Series of Potent Selective Cannabinoid Receptor 2 Inverse Agonists: Design, Synthesis, and Binding Mode Prediction. Philippe Diaz, Sharangdhar S. PhatakJijun Xu, Fanny Astruc Diaz, Claudio N. Cavasotto, Mohamed Naguib. J.Med.Chem. 2009, 52 (2), 433-444.

MDA7, a novel selective cannabinoid receptor 2 agonist preventing allodynia in rats with neuropathic painNaguib, M.; Diaz, P.; XuJJ.; Astruc-Diaz, F.; Craig, S.; Brown, DL. Br.J.Pharmacol. 2008, 155 (7), 1104-1116.

Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective CB2 agonists for the treatment of neuropathic pain. Philippe Diaz, Jijun Xu, Fanny Astruc Diaz, Hao-Min Pan, David L. Brown, Mohamed Naguib. J.Med.Chem. 2008, 51, 4932–4947.

Efficient synthetic approach to heterocycles possessing the 3,3-disubstituted-2,3-dihydrobenzofuran skeleton via diverse palladium-catalyzed tandem reactionsSzlosek-Pinaud, M.; Diaz, P.; Martinez, J.; Lamaty, F. Tetrahedron. 2007, 63, 3340–3349.

Solid-phase synthesis of diaryl sulfides: Direct coupling of solid supported aryl halides with thiols using an insoluble polymer supported reagentGendre, F.; Yang, M.; Diaz, P. Org. Lett. 2005, 7 (13), 2719–2722.

Palladium-catalyzed cascade allylation / carbopalladation / cross coupling: a novel three-component reaction for the synthesis of 3,3-disubstituted-2,3-dihydrobenzofuransSzlosek-Pinaud, M.; Diaz, P.; Martinez, J.; Lamaty, F. Tetrahedron Lett. 2003, 44, 8657–8659.

Solution-Phase Synthesis of Diaryl Selenides using Polymer Supported BorohydrideMillois, C.; Diaz, P. Org. Lett. 2000, 2 (12), 1705-1708.

Coupling reaction of chalcogenyl halides with alkynes on solid support. Synthesis of new selenium-containing retinoidsGendre, F.; Diaz, P. Tetrahedron Lett. 2000, 41, 5193-5197.

New Selenium-Containing Acetylenic Retinoids by Direct Coupling of Alkynylsilanes with Selenylhalides. Diaz, P.; Gendre, F.; Bernardon, J.M. Tetrahedron Lett. 1998, 39, 9003-9006.

New Synthetic Retinoids obtained by a Tandem Cyclisation-Anion Capture Process. Diaz, P.; Gendre, F.; Stella,L.; Charpentier, B. Tetrahedron, 1998, 54, 4579-4590.


The University of Montana-Missoula
The Department of Biomedical & Pharmaceutical Sciences
32 Campus Drive, Skaggs 395
Missoula, MT 59812-1552
Phone 406.243.4767 Fax: 406.243.5228
Email: biomed@umontana.edu

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