Synthesis of Novel GABA Uptake Inhibitors. 4.1Bioisosteric Transformation and Successive Optimization of Known GABA Uptake Inhibitors Leading to a Series of Potent Anticonvulsant Drug Candidates

Knud Erik Andersen; Jan L. Sørensen; Per O. Huusfeldt; Lars J. S. Knutsen; Jesper Lau; Behrend F. Lundt; Hans Petersen; Peter D. Suzdak; Michael D. B. Swedberg

doi:10.1021/jm980492e

Synthesis of Novel GABA Uptake Inhibitors. 4.1Bioisosteric Transformation and Successive Optimization of Known GABA Uptake Inhibitors Leading to a Series of Potent Anticonvulsant Drug Candidates

Journal of Medicinal Chemistry ◽

10.1021/jm980492e ◽

1999 ◽

Vol 42 (21) ◽

pp. 4281-4291 ◽

Cited By ~ 32

Author(s):

Knud Erik Andersen ◽

Jan L. Sørensen ◽

Per O. Huusfeldt ◽

Lars J. S. Knutsen ◽

Jesper Lau ◽

...

Keyword(s):

Anticonvulsant Drug ◽

Gaba Uptake ◽

Drug Candidates ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors ◽

Successive Optimization

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The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (Tiagabine) as an anticonvulsant drug candidate

Journal of Medicinal Chemistry ◽

10.1021/jm00064a005 ◽

1993 ◽

Vol 36 (12) ◽

pp. 1716-1725 ◽

Cited By ~ 122

Author(s):

Knud Erik Andersen ◽

Claus Braestrup ◽

Frederik C. Groenwald ◽

Anker S. Joergensen ◽

Erik B. Nielsen ◽

...

Keyword(s):

Anticonvulsant Drug ◽

Drug Candidate ◽

Gaba Uptake ◽

Structure Activity ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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Synthesis and Biochemical Studies of Spirocyclic Amino Acid Esters, Part 3 Activity of 2-Azaspiro[4.5]decane-6-carboxylates as GABA-Uptake Inhibitors

Archiv der Pharmazie ◽

10.1002/ardp.19963290307 ◽

1996 ◽

Vol 329 (3) ◽

pp. 149-154 ◽

Cited By ~ 4

Author(s):

Wilhelm Fleischhacker ◽

Silvia Lauritz ◽

Ernst Urban ◽

Peter Baumann ◽

Helmut Bittiger

Keyword(s):

Amino Acid ◽

Gaba Uptake ◽

Amino Acid Esters ◽

Uptake Inhibitors ◽

Biochemical Studies ◽

Gaba Uptake Inhibitors ◽

Acid Esters

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ChemInform Abstract: Design, Synthesis and Evaluation of Substituted Triarylnipecotic Acid Derivatives as GABA Uptake Inhibitors: Identification of a Ligand with Moderate Affinity and Selectivity for the Cloned Human GABA Transporter GAT-3.

ChemInform ◽

10.1002/chin.199451176 ◽

2010 ◽

Vol 25 (51) ◽

pp. no-no

Author(s):

T. G. M. DHAR ◽

L. A. BORDEN ◽

S. TYAGARAJAN ◽

K. E. SMITH ◽

T. A. BRANCHEK ◽

...

Keyword(s):

Gaba Uptake ◽

Gaba Transporter ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2009.08.010 ◽

2009 ◽

Vol 17 (18) ◽

pp. 6540-6546 ◽

Cited By ~ 9

Author(s):

Weiping Zhuang ◽

Xueqing Zhao ◽

Gang Zhao ◽

Lihe Guo ◽

Yunyang Lian ◽

...

Keyword(s):

Acetic Acid ◽

Biological Evaluation ◽

Gaba Uptake ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2019.01.024 ◽

2019 ◽

Vol 27 (5) ◽

pp. 822-831 ◽

Cited By ~ 1

Author(s):

Krisztián Tóth ◽

Georg Höfner ◽

Klaus T. Wanner

Keyword(s):

Biological Evaluation ◽

Gaba Uptake ◽

Nipecotic Acid ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Anticonvulsant Profiles of the Potent and Orally Active GABA Uptake Inhibitors SK&F 89976-A and SK&F 100330-A and Four Prototype Antiepileptic Drugs in Mice and Rats

Epilepsia ◽

10.1111/j.1528-1157.1991.tb04694.x ◽

1991 ◽

Vol 32 (4) ◽

pp. 569-577 ◽

Cited By ~ 20

Author(s):

Ewart A. Swinyard ◽

H. Steve White ◽

Harold H. Wolf ◽

William E. Bondinell

Keyword(s):

Antiepileptic Drugs ◽

Gaba Uptake ◽

Uptake Inhibitors ◽

Orally Active ◽

Gaba Uptake Inhibitors

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GABA-A agonists and GABA uptake inhibitors: Structure-activity relationships

Drug Development Research ◽

10.1002/ddr.430210304 ◽

1990 ◽

Vol 21 (3) ◽

pp. 169-188 ◽

Cited By ~ 25

Author(s):

Erik Falch ◽

Orla M. Larsson ◽

Arne Schousboe ◽

Povl Krogsgaard-Larsen

Keyword(s):

Gaba Uptake ◽

Gaba A ◽

Structure Activity Relationships ◽

Structure Activity ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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ChemInform Abstract: Synthesis and Biochemical Studies of Spirocyclic Amino Acid Esters. Part 3. Activity of 2-Azaspiro(4.5)decane-6-carboxylates as GABA- Uptake Inhibitors.

ChemInform ◽

10.1002/chin.199628152 ◽

2010 ◽

Vol 27 (28) ◽

pp. no-no

Author(s):

W. FLEISCHHACKER ◽

S. LAURITZ ◽

E. URBAN ◽

P. BAUMANN ◽

H. BITTIGER

Keyword(s):

Amino Acid ◽

Gaba Uptake ◽

Amino Acid Esters ◽

Uptake Inhibitors ◽

Biochemical Studies ◽

Gaba Uptake Inhibitors ◽

Acid Esters

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Comparative effects of the GABA uptake inhibitors, tiagabine and NNC-711, on extracellular GABA levels in the rat ventrolateral thalamus

Neurochemical Research ◽

10.1007/bf02529130 ◽

1996 ◽

Vol 21 (2) ◽

pp. 135-140 ◽

Cited By ~ 27

Author(s):

D. A. Richards ◽

N. G. Bowery

Keyword(s):

Gaba Uptake ◽

Uptake Inhibitors ◽

Ventrolateral Thalamus ◽

Gaba Uptake Inhibitors

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Biochemical and behavioral studies following subchronic administration of GABA uptake inhibitors in mice

Neuropharmacology ◽

10.1016/0028-3908(91)90164-7 ◽

1991 ◽

Vol 30 (11) ◽

pp. 1187-1192 ◽

Cited By ~ 8

Author(s):

E Karbon

Keyword(s):

Gaba Uptake ◽

Uptake Inhibitors ◽

Behavioral Studies ◽

Gaba Uptake Inhibitors

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