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Abstract

The lipophilicity of thirty-two novel acetylcholinesterase (AChE) inhibitors — 1,2,3,4-tetrahydroacridine and 2,3-dihydro-1H-cyclopenta[b]quinoline derivatives was studied by thin layer chromatography. The analyzed compounds were chromatographed on RP-18, RP-8, RP-2, CN and NH2 stationary phases with dioxane — citric buffer pH 3.0 binary mobile phases containing different proportions of dioxane. RM values for pure water were extrapolated from the linear Soczewiński-Wachtmeister equation and six compounds with known literature log P values were used as reference calibration data set for computation of experimental log P values. The obtained results were compared with computationally calculated partition coefficients values (AlogPs, AClogP, AlogP, MlogP, KOWWIN, XlogP2, XlogP3) by PCA and significant differences between them were observed.

rat liver sulfotransferase gene expression. Drug Metabol. Dispos. , 23(4), 455-459. Tomlinson, D. R., Gardiner, N. J. (2008). Glucose neurotoxicity. Nat. Rev. Neurosci. , 9(1), 36-45. Tracy, J. A., Dyck, P. J. (2008). The spectrum of diabetic neuropathies. Phys. Med. Rehabil. Clin. N. Amer. , 19(1), 1-26. Tyagi, E., Agrawal, R., Nath, C., Shukla, R. (2007). Effect of anti-dementia drugs on LPS induced neuroinflammation in mice. Life Sci. , 80(21), 1977-1983. Wang, W., Wang, Y. P., Hu, G. Y. (2004). Tetrahydroacridine inhibits voltage-dependent Na(+) current in

, T. E.; El-Kazak, A. M.: Synthesis and antimicrobial activity of some new 1,3-thiazoles, 1,3,4-thiadiazoles, 1,2,4-triazoles and 1,3-thiazines incorporating acridine and 1,2,3,4-tetrahydroacridine moieties. Eur. J. Chem. 1 (2010) 6–11. 10.5155/eurjchem.1.1.6-11.12 Ali T. E. El-Kazak A. M. Synthesis and antimicrobial activity of some new 1,3-thiazoles, 1,3,4-thiadiazoles, 1,2,4-triazoles and 1,3-thiazines incorporating acridine and 1,2,3,4-tetrahydroacridine moieties Eur. J. Chem. 1 2010 6 11 7 Li, S. H.; Li, G.; Huang, H. M.; Xiong, F.; Mai, X.; Kuang, B. H.; Liu

Universit t Berlin 3 Abteilung jur Neurologie und Psychiatrie, Fachkrankenhaus Lichtenberg, Berlin 4 Institut f r Neuropathologie, Klinikum Steglitz, Freie Universit t Berlin (Received March 20/June 11, 1991) Summary: Galanthamine, physostigmine and 9-amino-l,2,3,4-tetrahydroacridine (tacrine) were evaluated s inhibitors of human acetylcholinesterase activity from samples of postmortem human brain, fresh brain cortex biopsies and human erythrocytes. Acetylcholinesterase activity was most effectively inhibited in all tissues by physostigmine, followed by tacrine and

starting aniline (C n F 2n+1 ). These reactions are exemplified in Scheme 5 by the synthesis of 4-(perfluoropropyl)quinolines 44 – 47 by treatment of 2-(perfluorobutyl)aniline (2, n=4, R 1 = H) with various lithium enolates of ketones and by LDA-mediated electrocyclization of the corresponding ketimines 48 and 49 [32]. Scheme 5 Synthesis of acridines Base-mediated cyclization of a ketimine derived from 2-(trifluoromethyl)aniline ( 2 , n=1) and an acyclic ketone furnishes a quinoline, as discussed above, but a 1,2,3,4-tetrahydroacridine 51 [31] is produced in a

, Renou J, Sanson B, Colletier JP, Arboléas M, Loiodice M, Weik M, Jean L, Renard P-Y, Nachon F, Baati R. Design, synthesis and biological evaluation of novel tetrahydroacridine pyridinealdoxime and -amidoxime hybrids as efficient uncharged reactivatorsofnerveagent-inhibitedhumanacetylcholinesterase. Eur J Med Chem 2014;78:455-67. doi: 10.1016/j.ejmech.2014.03.044 39. Kovarik Z, Maček N, Sit RK, Radić Z, Fokin VV, Sharpless KB. Taylor P. Centrally acting oximes in reactivation of tabun-phosphoramidated AChE. Chem Biol Interact 2013;203:77-80. doi: 10.1016/j.cbi.2012

.048, wRref(F2) = 0.056, T = 298 K. Source of material The compound was synthesized as described by us in [1]. The recrystallization was done from methylene chloride. Discussion Tetrahydroaminoacridine (THA, Cognex) [2] has been the first approval drug for the treatment of Alzheimer’s Disease AD. Since this period, Acetylcholine Esterase Inhibitors (AcHEI) de- rived from tetrahydroacridine, like Tacrine-Huperzine A (Huprines) [3], have been under consideration. In an attempt to obtain potent AchEI, we modified the saturated ring by introduc- ing a thiazolo supplementary

), a = 10.225(1) Â, b = 11.4840(9) Â, c = 12.019(1) A, a = 96.732(5)°, β = 99.616(4)°, γ = 102.884(4)°, V= 1338.8 Â3, Z = 4, Rgl(F) = 0.048, wR^F2) = 0.056, Τ = 298 Κ. Source of material The compound was synthesized as described by us in [1]. The recrystallization was done from methylene chloride. Discussion Tetrahydroaminoacridine (THA, Cognex) [2] has been the first approval drug for the treatment of Alzheimer's Disease AD. Since this period, Acetylcholine Esterase Inhibitors (AcHEI) de- rived from tetrahydroacridine, like Tacrine-Huperzine A (Huprines

activity of Prunus persica L. Batsch in rats J Mol Neurosci 2006 29 101 7 7. Szwajgier D, Borowiec K. Screening for cholinesterase inhibitors in selected fruits and vegetables. Electron J Pol Agric Univ 2012;15:#06. Szwajgier D Borowiec K Screening for cholinesterase inhibitors in selected fruits and vegetables Electron J Pol Agric Univ 2012 15 #06 8. Kim Y-K, Koo B-S, Gong D-J, Lee Y-C, Ko J-H, Kim C-H. Comparative effect of Prunus persica L. BATSCH-water extract and tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride) on concentration of extracellular

activity of 6-arylpyrido [2,3- d ]pyrimidin-7-amine derivatives J Med Chem 1981 24 382 [14] Brooks JR, Berman C, Hichens M, Primka RL, Reynolds GF, Ramusson GH. Biological activities of a new steroidal inhibitor of δ4-5α-reductase. Proc Soc Exp Biol Med. 1982;169:67. 10.3181/00379727-169-41309 Brooks JR Berman C Hichens M Primka RL Reynolds GF Ramusson GH Biological activities of a new steroidal inhibitor of δ 4 -5α-reductase Proc Soc Exp Biol Med 1982 169 67 [15] Rampa A, Bisi A, Belluti F, Cavalli A, Bartolini M, Cavrini V. SAR of 9-amino-1,2,3,4-tetrahydroacridine