Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the Excitatory Amino Acid Transporters (EAATs): improving the potency of a micromolar screening Hit is not truism

Activity Relationship ◽

Amino Acid Transporters ◽

Excitatory Amino Acid Transporters ◽

Structure Activity ◽

Relationship Study ◽

Potential Inhibitors

Identification and Structure–Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3)

ACS Chemical Neuroscience ◽

10.1021/acschemneuro.9b00447 ◽

2019 ◽

Vol 10 (10) ◽

pp. 4414-4429

Author(s):

Peng Wu ◽

Walden E. Bjørn-Yoshimoto ◽

Markus Staudt ◽

Anders A. Jensen ◽

Lennart Bunch

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Activity Relationship ◽

Selective Inhibitors ◽

Structure Activity ◽

Relationship Study ◽

Subtype 3

Correction to Chemoenzymatic Synthesis of New 2,4-syn-Functionalized (S)-Glutamate Analogues and Structure–Activity Relationship Studies at Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters

10.1021/jm400829s ◽

2013 ◽

Vol 56 (14) ◽

pp. 5985-5985 ◽

Cited By ~ 1

Author(s):

Zeinab Assaf ◽

Anja P. Larsen ◽

Raminta Venskutonytė ◽

Liwei Han ◽

Bjarke Abrahamsen ◽

...

Keyword(s):

Amino Acid ◽

Glutamate Receptors ◽

Excitatory Amino Acid ◽

Chemoenzymatic Synthesis ◽

Ionotropic Glutamate Receptors ◽

Activity Relationship ◽

Amino Acid Transporters ◽

Structure Activity ◽

Glutamate Analogues

Chemoenzymatic Synthesis of New 2,4-syn-Functionalized (S)-Glutamate Analogues and Structure–Activity Relationship Studies at Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters

10.1021/jm301433m ◽

2013 ◽

Vol 56 (4) ◽

pp. 1614-1628 ◽

Cited By ~ 30

Author(s):

Zeinab Assaf ◽

Anja P. Larsen ◽

Raminta Venskutonytė ◽

Liwei Han ◽

Bjarke Abrahamsen ◽

...

Keyword(s):

Amino Acid ◽

Glutamate Receptors ◽

Excitatory Amino Acid ◽

Chemoenzymatic Synthesis ◽

Ionotropic Glutamate Receptors ◽

Activity Relationship ◽

Amino Acid Transporters ◽

Structure Activity ◽

Glutamate Analogues

Structure−Activity Relationship Study of First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)

10.1021/jm1009154 ◽

2010 ◽

Vol 53 (19) ◽

pp. 7180-7191 ◽

Cited By ~ 82

Author(s):

Mette N. Erichsen ◽

Tri H. V. Huynh ◽

Bjarke Abrahamsen ◽

Jesper F. Bastlund ◽

Christoffer Bundgaard ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Selective Inhibitor ◽

Activity Relationship ◽

Structure Activity ◽

Relationship Study ◽

Acid Transporter

Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure–Activity Relationship Study

10.1021/acs.jmedchem.6b01058 ◽

2016 ◽

Vol 59 (19) ◽

pp. 8757-8770 ◽

Cited By ~ 11

Author(s):

Stinne W. Hansen ◽

Mette N. Erichsen ◽

Bingru Fu ◽

Walden E. Bjørn-Yoshimoto ◽

Bjarke Abrahamsen ◽

...

Keyword(s):

Amino Acid ◽

Excitatory Amino Acid ◽

Amino Acid Transporter ◽

Activity Relationship ◽

New Class ◽

Structure Activity ◽

Relationship Study ◽

Acid Transporter

Structure-activity relationship study of a series of caspase inhibitors containing γ-amino acid moiety for treatment of cholestatic liver disease

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2018.04.002 ◽

2018 ◽

Vol 28 (10) ◽

pp. 1874-1878 ◽

Cited By ~ 2

Author(s):

Jianfeng Mou ◽

Songliang Wu ◽

Zhi Luo ◽

Fengying Guo ◽

Haiying He ◽

...

Keyword(s):

Liver Disease ◽

Amino Acid ◽

Activity Relationship ◽

Cholestatic Liver Disease ◽

Acid Moiety ◽

Caspase Inhibitors ◽

Structure Activity ◽

Amino Acid Moiety ◽

Structure–activity relationship study of compounds binding to large amino acid transporter 1 (LAT1) based on pharmacophore modeling and in situ rat brain perfusion

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2012.11.014 ◽

2013 ◽

Vol 48 (3) ◽

pp. 523-531 ◽

Cited By ~ 26

Author(s):

Henna Ylikangas ◽

Lauri Peura ◽

Kalle Malmioja ◽

Jukka Leppänen ◽

Krista Laine ◽

...

Keyword(s):

Amino Acid ◽

Rat Brain ◽

Brain Perfusion ◽

Amino Acid Transporter ◽

Pharmacophore Modeling ◽

Activity Relationship ◽

Structure Activity ◽

Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids

Organic & Biomolecular Chemistry ◽

10.1039/b908286g ◽

2009 ◽

Vol 7 (18) ◽

pp. 3805 ◽

Cited By ~ 12

Author(s):

Tomohiro Tanaka ◽

Wataru Nomura ◽

Tetsuo Narumi ◽

Ai Esaka ◽

Shinya Oishi ◽

...

Keyword(s):

Amino Acids ◽

Amino Acid ◽

Aromatic Amino Acids ◽

Activity Relationship ◽

Amino Acid Residues ◽

Structure Activity ◽

Structure-activity relationship study of antioxidative peptides by QSAR modeling: the amino acid next to C -terminus affects the activity

Journal of Peptide Science ◽

10.1002/psc.1345 ◽

2011 ◽

Vol 17 (6) ◽

pp. 454-462 ◽

Cited By ~ 39

Author(s):

Yao-Wang Li ◽

Bo Li ◽

Jiguo He ◽

Ping Qian

Keyword(s):

Amino Acid ◽

Activity Relationship ◽

Qsar Modeling ◽

Structure Activity ◽

C Terminus ◽

Structure–Activity Relationship Study of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and Absolute Configurational Assignment Using Infrared and Vibrational Circular Dichroism Spectroscopy in Combination with ab Initio Hartree–Fock Calculations

10.1021/jm300345z ◽

2012 ◽

Vol 55 (11) ◽

pp. 5403-5412 ◽

Cited By ~ 20

Author(s):

Tri H. V. Huynh ◽

Irene Shim ◽

Henrik Bohr ◽

Bjarke Abrahamsen ◽

Birgitte Nielsen ◽

...

Keyword(s):

Amino Acid ◽

Ab Initio ◽

Excitatory Amino Acid ◽

Vibrational Circular Dichroism ◽

Activity Relationship ◽

Hartree Fock ◽

Structure Activity ◽

Configurational Assignment ◽