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Items: 1 to 20 of 323

1.

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.

Gemma S, Gabellieri E, Huleatt P, Fattorusso C, Borriello M, Catalanotti B, Butini S, De Angelis M, Novellino E, Nacci V, Belinskaya T, Saxena A, Campiani G.

J Med Chem. 2006 Jun 1;49(11):3421-5.

PMID:
16722663
2.

Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.

Camps P, El Achab R, Görbig DM, Morral J, Muñoz-Torrero D, Badia A, Eladi Baños J, Vivas NM, Barril X, Orozco M, Luque FJ.

J Med Chem. 1999 Aug 26;42(17):3227-42.

PMID:
10464010
3.

Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.

Savini L, Gaeta A, Fattorusso C, Catalanotti B, Campiani G, Chiasserini L, Pellerano C, Novellino E, McKissic D, Saxena A.

J Med Chem. 2003 Jan 2;46(1):1-4.

PMID:
12502352
4.

Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.

Camps P, Formosa X, Galdeano C, Gómez T, Muñoz-Torrero D, Scarpellini M, Viayna E, Badia A, Clos MV, Camins A, Pallàs M, Bartolini M, Mancini F, Andrisano V, Estelrich J, Lizondo M, Bidon-Chanal A, Luque FJ.

J Med Chem. 2008 Jun 26;51(12):3588-98. doi: 10.1021/jm8001313. Epub 2008 Jun 3.

PMID:
18517184
5.

Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.

Butini S, Campiani G, Borriello M, Gemma S, Panico A, Persico M, Catalanotti B, Ros S, Brindisi M, Agnusdei M, Fiorini I, Nacci V, Novellino E, Belinskaya T, Saxena A, Fattorusso C.

J Med Chem. 2008 Jun 12;51(11):3154-70. doi: 10.1021/jm701253t. Epub 2008 May 15.

PMID:
18479118
7.

Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.

Elsinghorst PW, Tanarro CM, Gütschow M.

J Med Chem. 2006 Dec 14;49(25):7540-4.

PMID:
17149883
8.

First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.

Elsinghorst PW, Cieslik JS, Mohr K, Tränkle C, Gütschow M.

J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18.

PMID:
17944454
9.

Synthesis and biological evaluation of tacrine-thiadiazolidinone hybrids as dual acetylcholinesterase inhibitors.

Dorronsoro I, Alonso D, Castro A, del Monte M, García-Palomero E, Martínez A.

Arch Pharm (Weinheim). 2005 Jan;338(1):18-23.

PMID:
15674800
10.

Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.

Hamulakova S, Janovec L, Hrabinova M, Spilovska K, Korabecny J, Kristian P, Kuca K, Imrich J.

J Med Chem. 2014 Aug 28;57(16):7073-84. doi: 10.1021/jm5008648. Epub 2014 Aug 12.

PMID:
25089370
11.

Synthesis of tacrine analogues and their structure-activity relationships.

Proctor GR, Harvey AL.

Curr Med Chem. 2000 Mar;7(3):295-302. Review.

PMID:
10637366
12.

Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.

Muñoz-Ruiz P, Rubio L, García-Palomero E, Dorronsoro I, del Monte-Millán M, Valenzuela R, Usán P, de Austria C, Bartolini M, Andrisano V, Bidon-Chanal A, Orozco M, Luque FJ, Medina M, Martínez A.

J Med Chem. 2005 Nov 17;48(23):7223-33.

PMID:
16279781
13.

Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.

Campiani G, Fattorusso C, Butini S, Gaeta A, Agnusdei M, Gemma S, Persico M, Catalanotti B, Savini L, Nacci V, Novellino E, Holloway HW, Greig NH, Belinskaya T, Fedorko JM, Saxena A.

J Med Chem. 2005 Mar 24;48(6):1919-29.

PMID:
15771436
14.

[Design, synthesis and evaluation of tacrine-methoxybenzene hybrids as cholinesterases inhibitors].

Luo W, Zhao YM, Zhang Z, Su YB, Wang CJ.

Yao Xue Xue Bao. 2012 Jul;47(7):916-21. Chinese.

PMID:
22993857
15.

NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity.

Chen Y, Sun J, Huang Z, Liao H, Peng S, Lehmann J, Zhang Y.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3162-5. doi: 10.1016/j.bmcl.2013.04.008. Epub 2013 Apr 10.

PMID:
23639542
16.

Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation.

Luo W, Li YP, He Y, Huang SL, Tan JH, Ou TM, Li D, Gu LQ, Huang ZS.

Bioorg Med Chem. 2011 Jan 15;19(2):763-70. doi: 10.1016/j.bmc.2010.12.022. Epub 2010 Dec 13.

PMID:
21211982
17.
18.

New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties.

Fernández-Bachiller MI, Pérez C, Monjas L, Rademann J, Rodríguez-Franco MI.

J Med Chem. 2012 Feb 9;55(3):1303-17. doi: 10.1021/jm201460y. Epub 2012 Jan 27.

PMID:
22243648
19.

New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.

Camps P, El Achab R, Morral J, Muñoz-Torrero D, Badia A, Baños JE, Vivas NM, Barril X, Orozco M, Luque FJ.

J Med Chem. 2000 Nov 30;43(24):4657-66.

PMID:
11101357
20.

Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases.

Saxena A, Qian N, Kovach IM, Kozikowski AP, Pang YP, Vellom DC, Radić Z, Quinn D, Taylor P, Doctor BP.

Protein Sci. 1994 Oct;3(10):1770-8.

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