Polyneuropathy is a disease involving multiple peripheral nerves injuries. Axon regrowth remains the major prerequisite for plasticity, regeneration, circuit formation, and eventually functional recovery and therefore, regulation of neurite outgrowth might be a candidate for treating polyneuropathies. In a recent study, we synthesized and established the methylene-cycloalkylacetate (MCAs) pharmacophore as a lead for the development of a neurotropic drug (inducing neurite/axonal outgrowth) using the PC12 neuronal model. In the present study we extended the characterizations of the in vitro neurotropic effect of the derivative allylmethylene-cyclohexyl-propanoic acid (MCA-13) on dorsal root ganglia and spinal cord neuronal cultures and analyzed its safety properties using blood biochemistry and cell counting, acute toxicity evaluation in mice and different in vitro “off-target” pharmacological evaluations. This MCA derivative deserves further preclinical mechanistic pharmacological characterizations including therapeutic efficacy in in vivo animal models of polyneuropathies, toward development of a clinically relevant neurotropic drug.

Lahiani, A., Hacham-Geula, D., Lankri, D., Cornell-Kennon, S., Schaefer, E. M., Tsvelikhovsky, D.,  Lazarovici, P. ACS Chem. Neurosci.  2020, 11, 17, 2577-89.

Tsvelikhovsky Chem Eur J. Frontispiece


Tsvelikhovsky‚ D. ; Buchwald‚ S. L. (2011)

Concise Palladium-Catalyzed Synthesis of Dibenzazepins and Structural Analogues, J. Am. Chem. Soc. 133‚ 14228

Tsvelikhovsky‚ D. ; Buchwald‚ S. L. (2010)

Synthesis of Heterocycles via Pd-Ligand Controlled Cyclization of 2-Chloro-N-(2-vinyl)aniline: Preparation of Carbazoles‚ Indoles‚ Dibenzazepins and Acridines, J. Am. Chem. Soc132‚ 14048

Highlighted in [Science & Tech] Chemical & Engineering News, 88(44), 2010

Rozin, L. ; Tsvelikhovsky‚ D.; Schwarzeb, M.; Schomackerb, R.; Fanun, M.; Blum, J. (2010)

Dependence of the Heck coupling in aqueous microemulsion by supported palladium acetate on the surfactant and on the hydrophobicity of the support, J. Mol. Catal. A-Chem. 323‚ 65.

Tsvelikhovsky, D.; Popov, I.; Gutkin, V.; Rozin, A.; Shvartsman, A.; Blum, J. (2009)

On the Involvement of Palladium Nanoparticles in the Heck and Suzuki Reactions, Eur. J. Org. Chem. 98

Tsvelikhovsky, D.; Pessing, D.; Avnir, D.; Blum, J. (2008)

Forcing a cis-Product by Matrix Imprinting: Heck Reaction Catalyzed by Palladium Acetate Entrapped within cis-Imprinted Sol-Gel Derived Silicates, Adv. Syn. Catal. 350, 2856

Highlighted in Synfacts, 2009, 4, 462.

Tsvelikhovsky, D.; Blum, J. (2008)

Three Phase Microemulsion/Sol-Gel System for Aqueous C-C Coupling of Hydrophobic Substrates, Eur. J. Org. Chem. 201

Tsvelikhovsky, D.; Schumann, H.; Blum, J. (2006)

Cerium(IV)-Promoted Ethylation of Schiff Bases by Triethylaluminum, SYNTHESIS, 11, 1819

Tsvelikhovsky, D.; Gelman, D.; Molander, G. A.; Blum, J. (2004)

Lanthanide-Promoted Ethylation of Schiff Bases by Triethylaluminum, Org. Lett. 6, 1995

Gelman, D.; Tsvelikhovsky, D.; Molander, G. A.; Blum, J. (2002)

Palladium-Catalyzed Cross-Alkynylation of Aryl Bromides by Sodium Tetraalkynylaluminates, J. Org. Chem. 67, 6287


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