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Harold Kohn

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Amber M King; Cindy Barbosa; Theodore R Cummins; Michael R Due; Erik T Dustrude; Rajesh Khanna; Andrew D Piekarz; Christophe Salome; Yuying Wang; Fletcher White; Sarah M Wilson; Xiao-Fang Yang; Harold Kohn
Identification of the benzyloxyphenyl pharmacophore: a structural unit that promotes sodium channel slow inactivation.
Pranjal K Baruah; Marc De Ryck; Jason Dinsmore; Rafal Kaminski; Amber M King; Laurent Provins; Christophe Salome; Harold Kohn
Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides.
Amber M King; Marc De Ryck; Rafal Kaminski; James P Stables; Anne Valade; Harold Kohn
Defining the structural parameters that confer anticonvulsant activity by the site-by-site modification of (R)-N'-benzyl 2-amino-3-methylbutanamide.

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2012: Amber M King; Cindy Barbosa; Theodore R Cummins; Michael R Due; Erik T Dustrude; Rajesh Khanna; Andrew D Piekarz; Christophe Salome; Yuying Wang; Fletcher White; Sarah M Wilson; Xiao-Fang Yang; Harold Kohn
Identification of the benzyloxyphenyl pharmacophore: a structural unit that promotes sodium channel slow inactivation.
ACS chemical neuroscience 2012;3(12):1037-49.
2012: Pranjal K Baruah; Marc De Ryck; Jason Dinsmore; Rafal Kaminski; Amber M King; Laurent Provins; Christophe Salome; Harold Kohn
Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides.
Bioorganic & medicinal chemistry 2012;20(11):3551-64.
2011: Amber M King; Marc De Ryck; Rafal Kaminski; James P Stables; Anne Valade; Harold Kohn
Defining the structural parameters that confer anticonvulsant activity by the site-by-site modification of (R)-N'-benzyl 2-amino-3-methylbutanamide.
Journal of medicinal chemistry 2011;54(19):6432-42.
2011: Amber M King; Marc De Ryck; Rafal Kaminski; Christophe Salome; Elise Salomé-Grosjean; James P Stables; Anne Valade; Harold Kohn
Primary amino acid derivatives: substitution of the 4'-N'-benzylamide site in (R)-N'-benzyl 2-amino-3-methylbutanamide, (R)-N'-benzyl 2-amino-3,3-dimethylbutanamide, and (R)-N'-benzyl 2-amino-3-methoxypropionamide provides potent anticonvulsants with pain-attenuating properties.
Journal of medicinal chemistry 2011;54(19):6417-31.
2011: Ki Duk Park; Onrapak Reamtong; Rihe Liu; Claire Eyers; Simon J Gaskell; Dongwook Kim; Harold Kohn
Identification of a lacosamide binding protein using an affinity bait and chemical reporter strategy: 14-3-3 ζ.
Journal of the American Chemical Society 2011;133(29):11320-30.
2011: Amber M King; Marc De Ryck; Jason Dinsmore; Rafal Kaminski; Christophe Salome; Elise Salomé-Grosjean; Anne Valade; Harold Kohn
Primary amino acid derivatives: compounds with anticonvulsant and neuropathic pain protection activities.
Journal of medicinal chemistry 2011;54(13):4815-30.
2010: Pierre Morieux; Christophe Salome; Ki Duk Park; James P Stables; Harold Kohn
The structure-activity relationship of the 3-oxy site in the anticonvulsant (R)-N-benzyl 2-acetamido-3-methoxypropionamide.
Journal of medicinal chemistry 2010;53(15):5716-26.
2010: Ki Duk Park; James P Stables; Rihe Liu; Harold Kohn
Proteomic searches comparing two (R)-lacosamide affinity baits: An electrophilic arylisothiocyanate and a photoactivated arylazide group.
Organic & biomolecular chemistry 2010;8(12):2803-13.
2010: Christophe Salome; Elise Salomé-Grosjean; James P Stables; Harold Kohn
Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.
Journal of medicinal chemistry 2010;53(9):3756-71.
2010: Christophe Salome; Elise Salomé-Grosjean; Ki Duk Park; Pierre Morieux; Robert Swendiman; Erica DeMarco; James P Stables; Harold Kohn
Synthesis and anticonvulsant activities of (R)-N-(4'-substituted)benzyl 2-acetamido-3-methoxypropionamides.
Journal of medicinal chemistry 2010;53(3):1288-305.
2009: Ki Duk Park; Pierre Morieux; Christophe Salome; Steven W Cotten; Onrapak Reamtong; Claire Eyers; Simon J Gaskell; James P Stables; Rihe Liu; Harold Kohn
Lacosamide isothiocyanate-based agents: novel agents to target and identify lacosamide receptors.
Journal of medicinal chemistry 2009;52(21):6897-911.
2009: Ki Duk Park; Rihe Liu; Harold Kohn
Useful tools for biomolecule isolation, detection, and identification: acylhydrazone-based cleavable linkers.
Chemistry & biology 2009;16(7):763-72.
2009: Sang Hyup Lee; Harold Kohn
Nucleophilic activation of a tetra-substituted mitomycin cyclic bis-disulfide.
Chemical & pharmaceutical bulletin 2009;57(2):149-57.
2008: Pierre Morieux; James P Stables; Harold Kohn
Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives.
Bioorganic & medicinal chemistry 2008;16(19):8968-75.
2007: Thomas Stoehr; Harvey J Kupferberg; James P Stables; Daeock Choi; Robert H Harris; Harold Kohn; Nancy Walton; H White
Lacosamide, a novel anti-convulsant drug, shows efficacy with a wide safety margin in rodent models for epilepsy.
Epilepsy research 2007;74(2-3):147-54.
2006: Shuxing Zhang; Alexander Golbraikh; Scott Oloff; Harold Kohn; Alexander Tropsha
A novel automated lazy learning QSAR (ALL-QSAR) approach: method development, applications, and virtual screening of chemical databases using validated ALL-QSAR models.
Journal of chemical information and modeling 2006;46(5):1984-95.
2006: Boon-saeng Park; William R Widger; Harold Kohn
Fluorine-substituted dihydrobicyclomycins: synthesis and biochemical and biological properties.
Bioorganic & medicinal chemistry 2006;14(1):41-61.
2005: Gary E Duncan; Harold Kohn
The novel antiepileptic drug lacosamide blocks behavioral and brain metabolic manifestations of seizure activity in the 6 Hz psychomotor seizure model.
Epilepsy research 2005;67(1-2):81-7.
2005: Harold Kohn; William R Widger
The molecular basis for the mode of action of bicyclomycin.
Current drug targets. Infectious disorders 2005;5(3):273-95.
2005: Andrew P Brogan; William R Widger; Dalila Bensadek; Isabel Riba; Simon J Gaskell; Harold Kohn
Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.
Journal of the American Chemical Society 2005;127(8):2741-51.
2005: Andrew P Brogan; Jacob Verghese; William R Widger; Harold Kohn
Bismuth-dithiol inhibition of the Escherichia coli rho transcription termination factor.
Journal of inorganic biochemistry 2005;99(3):841-51.
2005: Pierre LeMagueres; Hookang Im; Jerry Ebalunode; Ulrich Strych; Michael J Benedik; James M Briggs; Harold Kohn; Kurt L Krause
The 1.9 A crystal structure of alanine racemase from Mycobacterium tuberculosis contains a conserved entryway into the active site.
Biochemistry 2005;44(5):1471-81.
2005: Sang Hyup Lee; Harold Kohn
7-N,7'-N'-(1",2"-Dithianyl-3",6"-dimethylenyl)bismitomycin C: synthesis and nucleophilic activation of a dimeric mitomycin.
Organic & biomolecular chemistry 2005;3(3):471-82.
2005: Emmanuel Skordalakes; Andrew P Brogan; Boon-saeng Park; Harold Kohn; James M Berger
Structural mechanism of inhibition of the Rho transcription termination factor by the antibiotic bicyclomycin.
Structure (London, England : 1993) 2005;13(1):99-109.
2004: Cécile Béguin; Arnaud LeTiran; James P Stables; Robert D Voyksner; Harold Kohn
N-Substituted amino acid N'-benzylamides: synthesis, anticonvulsant, and metabolic activities.
Bioorganic & medicinal chemistry 2004;12(11):3079-96.
2004: Myoung Goo Kim; Erik T Bodor; T Kendall Harden; Harold Kohn
C(8)-substituted 1-azabicyclo[3.3.1]non-3-enes: a novel scaffold for muscarinic receptor ligands.
Bioorganic & medicinal chemistry 2004;12(9):2357-67.
2004: Min Shen; Cécile Béguin; Alexander Golbraikh; James P Stables; Harold Kohn; Alexander Tropsha
Application of predictive QSAR models to database mining: identification and experimental validation of novel anticonvulsant compounds.
Journal of medicinal chemistry 2004;47(9):2356-64.
2004: Sang Hyup Lee; Harold Kohn
Cyclic disulfide C8 iminoporfiromycin: nucleophilic activation of a porfiromycin.
Journal of the American Chemical Society 2004;126(13):4281-92.
2003: Edwin Vedejs; B N Naidu; Artis Klapars; Don L Warner; Ven-shun Li; Younghwa Na; Harold Kohn
Synthetic enantiopure aziridinomitosenes: preparation, reactivity, and DNA alkylation studies.
Journal of the American Chemical Society 2003;125(51):15796-806.
2003: Cécile Béguin; Shridhar V Andurkar; Albert Y Jin; James P Stables; Donald F Weaver; Harold Kohn
Functionalized amido ketones: new anticonvulsant agents.
Bioorganic & medicinal chemistry 2003;11(19):4275-85.
2003: Thomas P Weber; William R Widger; Harold Kohn
Metal-1,4-dithio-2,3-dihydroxybutane chelates: novel inhibitors of the Rho transcription termination factor.
Biochemistry 2003;42(30):9121-6.
2003: Andrew P Brogan; William R Widger; Harold Kohn
Bicyclomycin fluorescent probes: synthesis and biochemical, biophysical, and biological properties.
The Journal of organic chemistry 2003;68(14):5575-87.
2003: Myoung Goo Kim; Erik T Bodor; Chen Wang; T Kendall Harden; Harold Kohn
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.
Journal of medicinal chemistry 2003;46(11):2216-26.
2003: Yi Xu; Jerry Johnson; Harold Kohn; William R Widger
ATP binding to Rho transcription termination factor. Mutant F355W ATP-induced fluorescence quenching reveals dynamic ATP binding.
The Journal of biological chemistry 2003;278(16):13719-27.
2003: Thomas P Weber; William R Widger; Harold Kohn
Metal dependency for transcription factor rho activation.
Biochemistry 2003;42(6):1652-9.
2003: Myoung Goo Kim; Ulrich Strych; Kurt Krause; Michael J Benedik; Harold Kohn
N(2)-substituted D,L-cycloserine derivatives: synthesis and evaluation as alanine racemase inhibitors.
The Journal of antibiotics 2003;56(2):160-8.
2002: Thomas P Weber; William R Widger; Harold Kohn
The Mg2+ requirements for rho transcription termination factor: catalysis and bicyclomycin inhibition.
Biochemistry 2002;41(41):12377-83.
2002: Arnaud LeTiran; James P Stables; Harold Kohn
Design and evaluation of affinity labels of functionalized amino acid anticonvulsants.
Journal of medicinal chemistry 2002;45(21):4762-73.
2002: Yi Xu; Harold Kohn; William R Widger
Mutations in the rho transcription termination factor that affect RNA tracking.
The Journal of biological chemistry 2002;277(33):30023-30.
2002: Min Shen; Arnaud LeTiran; Yunde Xiao; Alexander Golbraikh; Harold Kohn; Alexander Tropsha
Quantitative structure-activity relationship analysis of functionalized amino acid anticonvulsant agents using k nearest neighbor and simulated annealing PLS methods.
Journal of medicinal chemistry 2002;45(13):2811-23.
2002: Younghwa Na; Shuang Wang; Harold Kohn
7-N-(mercaptoalkyl)mitomycins: implications of cyclization for drug function.
Journal of the American Chemical Society 2002;124(17):4666-77.
2002: Sang Hyup Lee; Harold Kohn
Efficient synthesis of medium-sized cyclic ether diamines.
The Journal of organic chemistry 2002;67(5):1692-5.
2001: M Zewail-Foote; V S Li; Harold Kohn; David J Bearss; M Guzman; Laurence H Hurley
The inefficiency of incisions of ecteinascidin 743-DNA adducts by the UvrABC nuclease and the unique structural feature of the DNA adducts can be used to explain the repair-dependent toxicities of this antitumor agent.
Chemistry & biology 2001;8(11):1033-49.
2001: Y Na; V S Li; Y Nakanishi; Kenneth F Bastow; Harold Kohn
Synthesis, DNA cross-linking activity, and cytotoxicity of dimeric mitomycins.
Journal of medicinal chemistry 2001;44(21):3453-62.
2001: Arnaud LeTiran; James P Stables; Harold Kohn
Functionalized amino acid anticonvulsants: synthesis and pharmacological evaluation of conformationally restricted analogues.
Bioorganic & medicinal chemistry 2001;9(10):2693-708.
2001: Shridhar V Andurkar; Cécile Béguin; James P Stables; Harold Kohn
Synthesis and structural studies of aza analogues of functionalized amino acids: new anticonvulsant agents.
Journal of medicinal chemistry 2001;44(9):1475-8.
2001: Fabien Vincent; J Srinivasan; A Santillán; William R Widger; Harold Kohn
C(5)-C(5a)-modified bicyclomycins: synthesis, structure, and biochemical and biological properties.
The Journal of organic chemistry 2001;66(7):2251-64.
2001: V S Li; M S Tang; Harold Kohn
The effect of C(5) cytosine methylation at CpG sequences on mitomycin-DNA bonding profiles.
Bioorganic & medicinal chemistry 2001;9(4):863-73.
2000: Fabien Vincent; M Openshaw; M Trautwein; Simon J Gaskell; Harold Kohn; William R Widger
Rho transcription factor: symmetry and binding of bicyclomycin.
Biochemistry 2000;39(31):9077-83.
2000: Fabien Vincent; William R Widger; M Openshaw; Simon J Gaskell; Harold Kohn
5a-formylbicyclomycin: studies on the bicyclomycin-Rho interaction.
Biochemistry 2000;39(31):9067-76.
2000: V S Li; M Reed; Y Zheng; Harold Kohn; M Tang
C5 cytosine methylation at CpG sites enhances sequence selectivity of mitomycin C-DNA bonding.
Biochemistry 2000;39(10):2612-8.
1999: Shridhar V Andurkar; James P Stables; Harold Kohn
The anticonvulsant activities of N-benzyl 3-methoxypropionamides.
Bioorganic & medicinal chemistry 1999;7(11):2381-9.
1999: A Magyar; X Zhang; F Abdi; Harold Kohn; William R Widger
Identifying the bicyclomycin binding domain through biochemical analysis of antibiotic-resistant rho proteins.
The Journal of biological chemistry 1999;274(11):7316-24.
1999: S Wang; Harold Kohn
Studies on the mode of action of mitomycin C(7) aminoethylene disulfides (BMS-181174 and KW-2149): reactivity of 7-N-(mercaptoethyl)mitomycin C.
Journal of medicinal chemistry 1999;42(5):788-90.
1998: I Riba; Simon J Gaskell; H Cho; William R Widger; Harold Kohn
Evidence for the location of bicyclomycin binding to the Escherichia coli transcription termination factor Rho.
The Journal of biological chemistry 1998;273(51):34033-41.
1998: A Santillán; X Zhang; J Hardesty; William R Widger; Harold Kohn
Role of the C(6)-hydroxy group in bicyclomycin: synthesis, structure, and chemical, biochemical, and biological properties.
Journal of medicinal chemistry 1998;41(7):1185-94.
1996: D Choi; J P Stables; Harold Kohn
The anticonvulsant activities of functionalized N-benzyl 2-acetamidoacetamides. The importance of the 2-acetamido substituent.
Bioorganic & medicinal chemistry 1996;4(12):2105-14.
1996: A Magyar; X Zhang; Harold Kohn; William R Widger
The antibiotic bicyclomycin affects the secondary RNA binding site of Escherichia coli transcription termination factor Rho.
The Journal of biological chemistry 1996;271(41):25369-74.
1996: D Choi; J P Stables; Harold Kohn
Synthesis and anticonvulsant activities of N-Benzyl-2-acetamidopropionamide derivatives.
Journal of medicinal chemistry 1996;39(9):1907-16.
1995: H G Park; X Zhang; H S Moon; A Zwiefka; K Cox; Simon J Gaskell; William R Widger; Harold Kohn
Bicyclomycin and dihydrobicyclomycin inhibition kinetics of Escherichia coli rho-dependent transcription termination factor ATPase activity.
Archives of biochemistry and biophysics 1995;323(2):447-54.
1995: V S Li; D Choi; M S Tang; Harold Kohn
Structural requirements for mitomycin C DNA bonding.
Biochemistry 1995;34(21):7120-6.
1994: P Bardel; A Bolanos; Harold Kohn
Synthesis and anticonvulsant activities of alpha-acetamido-N-benzylacetamide derivatives containing an electron-deficient alpha-heteroaromatic substituent.
Journal of medicinal chemistry 1994;37(26):4567-71.
1994: Harold Kohn; K N Sawhney; D W Robertson; J D Leander
Anticonvulsant properties of N-substituted alpha,alpha-diamino acid derivatives.
Journal of pharmaceutical sciences 1994;83(5):689-91.
1993: Harold Kohn; K N Sawhney; P Bardel; D W Robertson; J D Leander
Synthesis and anticonvulsant activities of alpha-heterocyclic alpha-acetamido-N-benzylacetamide derivatives.
Journal of medicinal chemistry 1993;36(22):3350-60.
1993: A Zwiefka; Harold Kohn; William R Widger
Transcription termination factor rho: the site of bicyclomycin inhibition in Escherichia coli.
Biochemistry 1993;32(14):3564-70.
1991: Harold Kohn; K N Sawhney; P LeGall; D W Robertson; J D Leander
Preparation and anticonvulsant activity of a series of functionalized alpha-heteroatom-substituted amino acids.
Journal of medicinal chemistry 1991;34(8):2444-52.
1990: C H Lee; Harold Kohn
Anticonvulsant properties of 3-oxo- and 3-imino-4-substituted 1,2,5-thiadiazolidine 1,1-dioxides.
Journal of pharmaceutical sciences 1990;79(8):716-8.
1990: Harold Kohn; K N Sawhney; P LeGall; J D Conley; D W Robertson; J D Leander
Preparation and anticonvulsant activity of a series of functionalized alpha-aromatic and alpha-heteroaromatic amino acids.
Journal of medicinal chemistry 1990;33(3):919-26.
1989: K N Sawhney; Harold Kohn
Mitomycin C analogues with a substituted hydrazine at position 7. Synthesis, spectral properties, and biological activity.
Journal of medicinal chemistry 1989;32(1):248-52.
1988: Harold Kohn; J D Conley; J D Leander
Marked stereospecificity in a new class of anticonvulsants.
Brain research 1988;457(2):371-5.
1987: P L Fishbein; Harold Kohn
Synthesis and antineoplastic activity of 1a-formyl and 1a-thioformyl derivatives of mitomycin C and 2-methylaziridine.
Journal of medicinal chemistry 1987;30(10):1767-73.
1987: J D Conley; Harold Kohn
Functionalized DL-amino acid derivatives. Potent new agents for the treatment of epilepsy.
Journal of medicinal chemistry 1987;30(3):567-74.
1985: S Cortes; Z K Liao; D Watson; Harold Kohn
Effect of structural modification of the hydantoin ring on anticonvulsant activity.
Journal of medicinal chemistry 1985;28(5):601-6.
1978: J H Arceneaux; Harold Kohn; M L Steenberg; J P Buckley
Syntheses and pharmacological activity of N-acyl-substituted imidazolidinethiones and thioimidazolines.
Journal of pharmaceutical sciences 1978;67(5):600-2.
1977: Harold Kohn; B A Kohn; M L Steenberg; J P Buckley
Syntheses and pharmacological activity of substituted imidazolidinethiones and thiomidazolines.
Journal of medicinal chemistry 1977;20(1):158-60.
1972: Harold Kohn; S J Benkovic; R A Olofson
Dependence of mechanism on pH for deuterium-hydrogen exchange in 1-methyltetrazole-5-d. Transition metal ion catalysis of a deprotonation process.
Journal of the American Chemical Society 1972;94(16):5759-65.