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Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors.
Szymanski P, Karpiński A, Mikiciuk-Olasik E. Szymanski P, et al. Eur J Med Chem. 2011 Aug;46(8):3250-7. doi: 10.1016/j.ejmech.2011.04.038. Epub 2011 Apr 22. Eur J Med Chem. 2011. PMID: 21570751
The compounds of interest were obtained from the reaction of activated 4-FBA and diamino derivatives of 1,2,3,4-tetrahydroacridine. The compounds C6-2KW/HCl, C6-4KW/HCl and C6-3KW/HCl have four-fold higher antiacetylcholinesterase activity than THA. ...
The compounds of interest were obtained from the reaction of activated 4-FBA and diamino derivatives of 1,2,3,4-tetrahy …
Purification of acetylcholinesterase by 9-amino-1,2,3,4-tetrahydroacridine from human erythrocytes.
Kaya HB, Özcan B, Şişecioğlu M, Ozdemir H. Kaya HB, et al. Appl Biochem Biotechnol. 2013 May;170(1):198-209. doi: 10.1007/s12010-013-0177-3. Epub 2013 Mar 15. Appl Biochem Biotechnol. 2013. PMID: 23494216
The acetylcholinesterase enzyme was purified from human erythrocyte membranes using a simple and effective method in a single step. Tacrine (9-amino-1,2,3,4-tetrahydroacridine) is a well-known drug for the treatment of Alzheimer's disease, which inhibits chol …
The acetylcholinesterase enzyme was purified from human erythrocyte membranes using a simple and effective method in a single step. Tacrine …
SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.
Recanatini M, Cavalli A, Belluti F, Piazzi L, Rampa A, Bisi A, Gobbi S, Valenti P, Andrisano V, Bartolini M, Cavrini V. Recanatini M, et al. J Med Chem. 2000 May 18;43(10):2007-18. doi: 10.1021/jm990971t. J Med Chem. 2000. PMID: 10821713
By means of the Hansch approach, QSAR equations were obtained, quantitatively accounting for both the detrimental steric effect of substituents in position 7 and the favorable electron-attracting effect exerted by substituents in positions 6 and 7 of the 9-amino-1,2 …
By means of the Hansch approach, QSAR equations were obtained, quantitatively accounting for both the detrimental steric effect of substitue …
9-[3-(2-Nitro-1-imidazolyl)propylamino]-1,2,3,4-tetrahydroacridine hydrochloride. A novel DNA-affinic hypoxic cell cytotoxin and radiosensitizer. Comparison with NLA-1.
Papadopoulou MV, Rosenzweig HS, Doddi M, Bloomer WD. Papadopoulou MV, et al. Oncol Res. 1994;6(9):439-48. Oncol Res. 1994. PMID: 7703530
Electron-affinic compounds with strong DNA intercalating properties have demonstrated less than the expected radiosensitization due to restriction of their mobility along the DNA backbone and their lower extravascular diffusion in tumors. A 2-nitroimidazole linked 1,2 …
Electron-affinic compounds with strong DNA intercalating properties have demonstrated less than the expected radiosensitization due to restr …
Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease.
Drukarch B, Leysen JE, Stoof JC. Drukarch B, et al. Life Sci. 1988;42(9):1011-7. doi: 10.1016/0024-3205(88)90431-6. Life Sci. 1988. PMID: 2893967
In a recent study we have documented the acetylcholinesterase and outward K+-current inhibiting activity of 9-amino-1,2,3,4-tetrahydroacridine (THA), a drug reportedly active in the treatment of Alzheimer patients. ...
In a recent study we have documented the acetylcholinesterase and outward K+-current inhibiting activity of 9-amino-1,2,3 …
9-Amino-1,2,3,4-tetrahydroacridine (THA) is a potent blocker of cardiac potassium channels.
Osterrieder W. Osterrieder W. Br J Pharmacol. 1987 Nov;92(3):521-5. doi: 10.1111/j.1476-5381.1987.tb11352.x. Br J Pharmacol. 1987. PMID: 2447986 Free PMC article.
1. 9-Amino-1,2,3,4-tetrahydroacridine (THA) is a compound with structural similarity to the K+ channel blocker 4-aminopyridine. ...
1. 9-Amino-1,2,3,4-tetrahydroacridine (THA) is a compound with structural similarity to the K+ channel blocker 4-aminop …
Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA) on ATP diphosphohydrolase (EC 3.6.1.5) and 5'-nucleotidase (EC 3.1.3.5) from rat brain synaptosomes.
Bonan CD, Battastini AM, Schetinger MR, Moreira CM, Frassetto SS, Dias RD, Sarkis JJ. Bonan CD, et al. Gen Pharmacol. 1997 May;28(5):761-6. doi: 10.1016/s0306-3623(96)00276-5. Gen Pharmacol. 1997. PMID: 9184816
1. 9-Amino-1,2,3,4-tetrahydroacridine (THA), an acetylcholinesterase inhibitor, significantly inhibited in vitro the ATP diphosphohydrolase activity of synaptosomes from the cerebral cortex and hippocampus of adult rats. 2. ...
1. 9-Amino-1,2,3,4-tetrahydroacridine (THA), an acetylcholinesterase inhibitor, significantly inhibited in vitro the AT …
Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines.
Cumming P, Vincent SR. Cumming P, et al. Biochem Pharmacol. 1992 Sep 1;44(5):989-92. doi: 10.1016/0006-2952(92)90133-4. Biochem Pharmacol. 1992. PMID: 1530666
Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). Structural fragments of tacrine were less potent inhibitors of rat brain HNMT than was …
Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1 …
50 results