ARTICLE;
CHOLINESTERASE INHIBITION;
DRUG BINDING;
DRUG DESIGN;
DRUG POTENCY;
DRUG SYNTHESIS;
ENZYME ACTIVE SITE;
HUMAN;
HYDROGEN BOND;
IC 50;
IN VITRO STUDY;
MOLECULAR DOCKING;
STRUCTURE ACTIVITY RELATION;
Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors
F. Leonetti, M. Catto, O. Nicolotti, L. Pisani, A. Cappa, A. Stefanachi, and A. Carotti Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors Bioorg. Med. Chem. 16 2008 7450 7456
Study of neuroprotection of donepezil, a therapy for Alzheimer's disease
S. Akasofu, M. Kimura, I. Kosasa, K. Sawada, and H. Ogura Study of neuroprotection of donepezil, a therapy for Alzheimer's disease Chem. Biol. Interact. 175 2008 222 226
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors
R. Sheng, X. Lin, J.Y. Li, Y.K. Jiang, Z.C. Shang, and Y.Z. Hu Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors Bioorg. Med. Chem. Lett. 15 2005 3834 3837
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B
X.-C. He, S. Feng, Z.-F. Wang, Y. Shi, S. Zheng, Y. Xia, H. Jiang, X.-C. Tang, and D. Bai Study on dual-site inhibitors of acetylcholinesterase: highly potent derivatives of bis- and bifunctional huperzine B Bioorg. Med. Chem. 15 2007 1394 1408
The synaptic protein neuroligin-1 interacts with the amyloid β-peptide. Is there a role in Alzheimer's disease?
M.C. Dinamarca, D. Weinstein, O. Monasterio, and N.C. Inestrosa The synaptic protein neuroligin-1 interacts with the amyloid β-peptide. Is there a role in Alzheimer's disease? Biochemistry 50 2011 8127 8137
Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors
H. Sugimoto, Y. Yamanishi, Y. Iimura, and Y. Kawakami Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors Curr. Med. Chem. 7 2000 303 339
Tacrine-based dual binding site acetylcholinesterase inhibitors as potential disease-modifying anti-Alzheimer drug candidates
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Galantamine and behavior in Alzheimer disease: Analysis of four trials
S. Kavanagh, M. Gaudig, B. Van Baelen, M. Adami, A. Delgado, C. Guzman, E. Jedenius, and B. Schaeuble Galantamine and behavior in Alzheimer disease: analysis of four trials Acta Neurol. Scand. 124 2011 302 308
Pharmacological activity and safety profile of P10358, a novel, orally active acetylcholinesterase inhibitor for Alzheimer's disease
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New multipotent tetracyclic tacrines with neuroprotective activity
J. Marco-Contelles, R. Leon, C. de los Rios, A.G. Garcia, M.G. Lopez, and M. Villarroya New multipotent tetracyclic tacrines with neuroprotective activity Bioorg. Med. Chem. 14 2006 8176 8185
Novel tacrine derivatives that block neuronal calcium channels
C. de los Rios, J.L. Marco, M.D.C. Carreiras, P.M. Chinchon, A.G. Garcia, and M. Villarroya Novel tacrine derivatives that block neuronal calcium channels Bioorg. Med. Chem. 10 2002 2077 2088
Synthesis and evaluation of substituted quinazolone derivatives for antibacterial, antifungal and antiacetylcholinesterase activities
A.K.S. Gupta, and H.K. Misra Synthesis and evaluation of substituted quinazolone derivatives for antibacterial, antifungal and antiacetylcholinesterase activities J. Pharm. Sci. 69 1980 1313 1317
Synthesis and anticholinesterase activity and cytotoxicity of novel amide derivatives
M.D. Altintop, Z.A. Kaplancikli, A. Ozdemir, G. Turan-Zitouni, H.E. Temel, and G. Akalin Synthesis and anticholinesterase activity and cytotoxicity of novel amide derivatives Arch. Pharm. 345 2012 112 116
Synthesis and potential muscarinic receptor binding and antioxidant properties of 3-(thiadiazolyl)pyridine 1-oxide compounds
A. Martinez, D. Alonso, A. Castro, V.J. Aran, I. Cardelus, J.E. Banos, and A. Badia Synthesis and potential muscarinic receptor binding and antioxidant properties of 3-(thiadiazolyl)pyridine 1-oxide compounds Arch. Pharm. 332 1999 191 194
Synthesis of 1-benzyl-4-2-(5-phenyl-1,3,4-thiadiazole-2-yl)aminoethyl piperidine as potential Alzheimer's disease modifying agent
D.N. Sarkandi, L. Firoozpour, A. Asadipour, V. Sheibani, M.A.M. Asli, A. Davood, A. Shafiee, and A. Foroumadi Synthesis of 1-benzyl-4-2-(5-phenyl-1,3,4- thiadiazole-2-yl)aminoethyl piperidine as potential Alzheimer's disease modifying agent Asian J. Chem. 23 2011 2503 2505
Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds
10.3109/14756366.2012.688041
A. Skrzypek, J. Matysiak, M.M. Karpińska, and A. Niewiadomy Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds J. Enzyme Inhib. Med. Chem. 2012 10.3109/14756366.2012.688041
Anticancer, neuroprotective activities and computational studies of 2-amino-1,3,4-thiadiazole based compound
W. Rzeski, J. Matysiak, and M. Kandefer-Szerszen Anticancer, neuroprotective activities and computational studies of 2-amino-1,3,4- thiadiazole based compound Bioorg. Med. Chem. 15 2007 3201 3207
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
C.A. Lipinski, F. Lombardo, B.W. Dominy, and P.J. Feeney Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Deliv. Rev. 23 1997 3 25
Chemical information management in drug discovery: Optimizing the computational and combinatorial chemistry interfaces
T.I. Oprea, J. Gottfries, V. Sherbukhin, P. Svensson, and T.C. Kuhler Chemical information management in drug discovery: optimizing the computational and combinatorial chemistry interfaces J. Mol. Graph. Model. 18 2000 512 524
Molecular properties that influence the oral bioavailability of drug candidates
D.F. Veber, S.R. Johnson, H.Y. Cheng, B.R. Smith, K.W. Ward, and K.D. Kopple Molecular properties that influence the oral bioavailability of drug candidates J. Med. Chem. 45 2002 2615 2623
Application of sulfinyl bis(2,4-dihydroxythiobenzoyl) in the synthesis of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles
J. Matysiak, and A. Niewiadomy Application of sulfinyl bis(2,4-dihydroxythiobenzoyl) in the synthesis of N-substituted 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles Synth. Commun. 36 2006 1621 1630
Synthesis and antiproliferative activity of some 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles
J. Matysiak, A. Nasulewicz, M. Pełczynska, M. Switalska, I. Jaroszewicz, and A. Opolski Synthesis and antiproliferative activity of some 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles Eur. J. Med. Chem. 41 2006 475 482
A new and rapid colorimetric determination of acetylcholinesterase activity
G.L. Ellman, K.D. Courtney, V. Andres, and R.M. Featherstone A new and rapid colorimetric determination of acetylcholinesterase activity Biochem. Pharmacol. 7 1961 88 95
Beta-amyloid aggregation induced by human acetylcholinesterase: Inhibition studies
M. Bartolini, C. Bertucci, V. Cavrini, and V. Andrisano Beta-amyloid aggregation induced by human acetylcholinesterase: inhibition studies Biochem. Pharmacol. 65 2003 407 416
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease
J. Marco-Contelles, R. Leon, C. de los Rios, A. Samadi, M. Bartolini, V. Andrisano, O. Huertas, X. Barril, F. Javier Luque, M.I. Rodriguez-Franco, B. Lopez, M.G. Lopez, A.G. Garcia, M. do Carmo Carreiras, and M. Villarroya Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease J. Med. Chem. 52 2009 2724 2732
Synthesis and antifungal activity of novel 5-substituted 4-(1,3,4-thiadiazol-2-yl)benzene-1,3-diols
J. Matysiak, A. Skrzypek, and A. Niewiadomy Synthesis and antifungal activity of novel 5-substituted 4-(1,3,4-thiadiazol-2-yl)benzene-1,3-diols Heteroat. Chem. 21 2010 533 540
2-(2,4-Dihydroxyphenyl)-1,3,4-thiadiazole analogues: Antifungal activity in vitro against Candida species
J. Matysiak, and Z. Malinski 2-(2,4-Dihydroxyphenyl)-1,3,4-thiadiazole analogues: antifungal activity in vitro against Candida species Russ. J. Bioorg. Chem. 33 2007 594 601
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties
P. Ertl, B. Rohde, and P. Selzer Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties J. Med. Chem. 43 2000 3714 3717
