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Boris Yagen

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Naama Hen; Meir Bialer; Boris Yagen
Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamates.
H Steve White; Karen S Wilcox; Boris Yagen; Anitha B Alex; Naama Hen; Dan Kaufmann; John H McDonough; Amanda Pollock; Tawfeeq Shekh-Ahmad; James P Stables; Meir Bialer
A new derivative of valproic acid amide possesses a broad-spectrum antiseizure profile and unique activity against status epilepticus and organophosphate neuronal damage.
Neta Pessah; Jakob Shimshoni; Bogdan Wlodarczyk; Boris Yagen; Richard H Finnell; Naama Hen; Meir Bialer
Design and pharmacological activity of glycinamide and N-methoxy amide derivatives of analogs and constitutional isomers of valproic acid.

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All Publications

2012: Naama Hen; Meir Bialer; Boris Yagen
Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamates.
Journal of medicinal chemistry 2012;55(6):2835-45.
2012: H Steve White; Karen S Wilcox; Boris Yagen; Anitha B Alex; Naama Hen; Dan Kaufmann; John H McDonough; Amanda Pollock; Tawfeeq Shekh-Ahmad; James P Stables; Meir Bialer
A new derivative of valproic acid amide possesses a broad-spectrum antiseizure profile and unique activity against status epilepticus and organophosphate neuronal damage.
Epilepsia 2012;53(1):134-46.
2011: Neta Pessah; Jakob Shimshoni; Bogdan Wlodarczyk; Boris Yagen; Richard H Finnell; Naama Hen; Meir Bialer
Design and pharmacological activity of glycinamide and N-methoxy amide derivatives of analogs and constitutional isomers of valproic acid.
Epilepsy & behavior : E&B 2011;22(3):461-8.
2011: Naama Hen; Meir Bialer; Boris Yagen; Alfonso Maresca; Mayank Aggarwal; Arthur H Robbins; Robert McKenna; Andrea Scozzafava; Claudiu T Supuran
Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV.
Journal of medicinal chemistry 2011;54(11):3977-81.
2010: Neta Pessah; Dan Kaufmann; Boris Yagen; Naama Hen; Bogdan Wlodarczyk; Richard H Finnell; Meir Bialer
Comparative pharmacodynamic and pharmacokinetic analysis of two anticonvulsant halo derivatives of 2,2,3,3-tetramethylcyclopropanecarboxamide, an amide of a cyclic analog of valproic acid.
Epilepsia 2010;51(10):1944-53.
2010: Dan Kaufmann; Boris Yagen; Anne Minert; Bogdan Wlodarczyk; Richard H Finnell; Volker Schurig; Marshall Devor; Meir Bialer
Evaluation of the antiallodynic, teratogenic and pharmacokinetic profile of stereoisomers of valnoctamide, an amide derivative of a chiral isomer of valproic acid.
Neuropharmacology 2010;58(8):1228-36.
2010: Naama Hen; Meir Bialer; Bogdan Wlodarczyk; Richard H Finnell; Boris Yagen
Syntheses and evaluation of anticonvulsant profile and teratogenicity of novel amide derivatives of branched aliphatic carboxylic acids with 4-aminobenzensulfonamide.
Journal of medicinal chemistry 2010;53(10):4177-86.
2010: Jakob A Shimshoni; Boris Yagen; Bogdan Wlodarczyk; Richard H Finnell; Volker Schurig; Meir Bialer
Evaluation of stereoselective anticonvulsant, teratogenic, and pharmacokinetic profile of valnoctylurea (capuride): a chiral stereoisomer of valproic acid urea derivative.
Epilepsia 2010;51(3):323-32.
2009: Dan Kaufmann; Meir Bialer; Jakob Shimshoni; Marshall Devor; Boris Yagen
Synthesis and evaluation of antiallodynic and anticonvulsant activity of novel amide and urea derivatives of valproic acid analogues.
Journal of medicinal chemistry 2009;52(22):7236-48.
2009: Akinobu Okada; Hiroko Noyori; Boris Yagen; Jakob Avi Shimshoni; Meir Bialer; Michio Fujiwara
Anticonvulsant profile and teratogenic evaluation of potent new analogues of a valproic acid urea derivative in NMRI mice.
Birth defects research. Part B, Developmental and reproductive toxicology 2009;86(5):394-401.
2009: Neta Pessah; Meir Bialer; Bogdan Wlodarczyk; Richard H Finnell; Boris Yagen
Alpha-fluoro-2,2,3,3-tetramethylcyclopropanecarboxamide, a novel potent anticonvulsant derivative of a cyclic analogue of valproic acid.
Journal of medicinal chemistry 2009;52(8):2233-42.
2008: Akinobu Okada; Yuko Onishi; Boris Yagen; Jakob Avi Shimshoni; Dan Kaufmann; Meir Bialer; Michio Fujiwara
Tetramethylcyclopropyl analogue of the leading antiepileptic drug, valproic acid: evaluation of the teratogenic effects of its amide derivatives in NMRI mice.
Birth defects research. Part A, Clinical and molecular teratology 2008;82(9):610-21.
2008: Jakob Avi Shimshoni; Boris Yagen; Neta Pessah; Bogdan Wlodarczyk; Richard Finnell; Meir Bialer
Anticonvulsant profile and teratogenicity of 3,3-dimethylbutanoylurea: a potential for a second generation drug to valproic acid.
Epilepsia 2008;49(7):1202-12.
2008: Jakob Avi Shimshoni; Meir Bialer; Boris Yagen
Synthesis and anticonvulsant activity of aromatic tetramethylcyclopropanecarboxamide derivatives.
Bioorganic & medicinal chemistry 2008;16(11):6297-305.
2008: Dan Kaufmann; Boris Yagen; Anne Minert; MICHAEL TAL; Marshall Devor; Meir Bialer
Evaluation of the enantioselective antiallodynic and pharmacokinetic profile of propylisopropylacetamide, a chiral isomer of valproic acid amide.
Neuropharmacology 2008;54(4):699-707.
2007: Jakob Shimshoni; Meir Bialer; Bogdan Wlodarczyk; Richard Finnell; Boris Yagen
Potent anticonvulsant urea derivatives of constitutional isomers of valproic acid.
Journal of medicinal chemistry 2007;50(25):6419-27.
2007: Jakob Shimshoni; Emma Dalton; A Jenkins; Sara Eyal; K Ewan; Robin S B Williams; N Pessah; Boris Yagen; Adrian J Harwood; Meir Bialer
The effects of central nervous system-active valproic acid constitutional isomers, cyclopropyl analogs, and amide derivatives on neuronal growth cone behavior.
Molecular pharmacology 2007;71(3):884-92.
2007: Meir Bialer; Boris Yagen
Valproic Acid: second generation.
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics 2007;4(1):130-7.
2007: Eyal Sobol; Boris Yagen; John G Lamb; H White; Bogdan Wlodarczyk; Richard Finnell; Meir Bialer
Anticonvulsant activity, neural tube defect induction, mutagenicity and pharmacokinetics of a new potent antiepileptic drug, N-methoxy-2,2,3,3-tetramethylcyclopropane carboxamide.
Epilepsy research 2007;73(1):75-84.
2006: Sara Eyal; John G Lamb; Misty Smith; Boris Yagen; E Fibach; Yoram Altschuler; H White; Meir Bialer
The antiepileptic and anticancer agent, valproic acid, induces P-glycoprotein in human tumour cell lines and in rat liver.
British journal of pharmacology 2006;149(3):250-60.
2006: Eyal Sobol; Boris Yagen; H Steve White; Karen S Wilcox; John G Lamb; Orit Pappo; Bogdan Wlodarczyk; Richard Finnell; Meir Bialer
Preclinical evaluation of 2,2,3,3-tetramethylcyclopropanecarbonyl-urea, a novel, second generation to valproic acid, antiepileptic drug.
Neuropharmacology 2006;51(4):933-46.
2006: Akinobu Okada; Yuko Onishi; Yoshinobu Aoki; Boris Yagen; Eyal Sobol; Meir Bialer; Michio Fujiwara
Teratology study of derivatives of tetramethylcyclopropyl amide analogues of valproic acid in mice.
Birth defects research. Part B, Developmental and reproductive toxicology 2006;77(3):227-33.
2005: Ilan Winkler; Eyal Sobol; Boris Yagen; Amir Steinman; Marshall Devor; Meir Bialer
Efficacy of antiepileptic tetramethylcyclopropyl analogues of valproic acid amides in a rat model of neuropathic pain.
Neuropharmacology 2005;49(8):1110-20.
2005: Eyal Sobol; Boris Yagen; Ilan Winkler; Malka Britzi; Dan Gibson; Meir Bialer
Pharmacokinetics and metabolism of a new potent antiepileptic drug, 2,2,3,3-tetramethycyclopropanecarbonylurea, in rats.
Drug metabolism and disposition: the biological fate of chemicals 2005;33(10):1538-46.
2005: Ilan Winkler; Simcha Blotnik; Jakob Shimshoni; Boris Yagen; Marshall Devor; Meir Bialer
Efficacy of antiepileptic isomers of valproic acid and valpromide in a rat model of neuropathic pain.
British journal of pharmacology 2005;146(2):198-208.
2005: Sara Eyal; Boris Yagen; Jakob Shimshoni; Meir Bialer
Histone deacetylases inhibition and tumor cells cytotoxicity by CNS-active VPA constitutional isomers and derivatives.
Biochemical pharmacology 2005;69(10):1501-8.
2004: Eyal Sobol; Meir Bialer; Boris Yagen
Tetramethylcyclopropyl analogue of a leading antiepileptic drug, valproic acid. Synthesis and evaluation of anticonvulsant activity of its amide derivatives.
Journal of medicinal chemistry 2004;47(17):4316-26.
2004: Sara Eyal; Boris Yagen; Eyal Sobol; Yoram Altschuler; Miriam Shmuel; Meir Bialer
The activity of antiepileptic drugs as histone deacetylase inhibitors.
Epilepsia 2004;45(7):737-44.
2004: Nina Isoherranen; René H Levy; Boris Yagen; José H Woodhead; H White; Meir Bialer
Metabolism of a new antiepileptic drug, N-methyl-tetramethylcyclopropanecarboxamide, and anticonvulsant activity of its metabolites.
Epilepsy research 2004;58(1):1-12.
2003: Nina Isoherranen; Ofer Spiegelstein; Meir Bialer; Jing Zhang; Michelle Merriweather; Boris Yagen; Michael Roeder; Aleata A Triplett; Volker Schurig; Richard Finnell
Developmental outcome of levetiracetam, its major metabolite in humans, 2-pyrrolidinone N-butyric acid, and its enantiomer (R)-alpha-ethyl-oxo-pyrrolidine acetamide in a mouse model of teratogenicity.
Epilepsia 2003;44(10):1280-8.
2003: Nina Isoherranen; H White; Brian D Klein; Michael Roeder; José H Woodhead; Volker Schurig; Boris Yagen; Meir Bialer
Pharmacokinetic-pharmacodynamic relationships of (2S,3S)-valnoctamide and its stereoisomer (2R,3S)-valnoctamide in rodent models of epilepsy.
Pharmaceutical research 2003;20(8):1293-301.
2003: Nina Isoherranen; Boris Yagen; Ofer Spiegelstein; Richard Finnell; Michelle Merriweather; José H Woodhead; Bogdan Wlodarczyk; H White; Meir Bialer
Anticonvulsant activity, teratogenicity and pharmacokinetics of novel valproyltaurinamide derivatives in mice.
British journal of pharmacology 2003;139(4):755-64.
2003: Nina Isoherranen; Boris Yagen; Ofer Spiegelstein; Amir Steinman; Richard Finnell; Meir Bialer
Gas chromatographic determination of novel valproyl taurinamide derivatives in mouse and dog plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 2003;788(1):125-36.
2003: Nina Isoherranen; Boris Yagen; Meir Bialer
New CNS-active drugs which are second-generation valproic acid: can they lead to the development of a magic bullet?
Current opinion in neurology 2003;16(2):203-11.
2003: Nina Isoherranen; Boris Yagen; José H Woodhead; Ofer Spiegelstein; Simcha Blotnik; Karen S Wilcox; Richard Finnell; Gregory D Bennett; H White; Meir Bialer
Characterization of the anticonvulsant profile and enantioselective pharmacokinetics of the chiral valproylamide propylisopropyl acetamide in rodents.
British journal of pharmacology 2003;138(4):602-13.
2002: Nina Isoherranen; H White; Richard Finnell; Boris Yagen; José H Woodhead; Gregory D Bennett; Karen S Wilcox; Matthew E Barton; Meir Bialer
Anticonvulsant profile and teratogenicity of N-methyl-tetramethylcyclopropyl carboxamide: a new antiepileptic drug.
Epilepsia 2002;43(2):115-26.
2001: M Wasserman; Boris Yagen; Simcha Blotnik; niv papo; Meir Bialer
Stereoselective pharmacokinetic analysis and antiepileptic activity of N-2-hydroxypropyl valpromide, a central nervous system--active chiral valproylamide.
Therapeutic drug monitoring 2001;23(4):414-20.
2001: Nina Isoherranen; Boris Yagen; Stefan Soback; Michael Roeder; Volker Schurig; Meir Bialer
Pharmacokinetics of levetiracetam and its enantiomer (R)-alpha-ethyl-2-oxo-pyrrolidine acetamide in dogs.
Epilepsia 2001;42(7):825-30.
2000: Ofer Spiegelstein; Boris Yagen; Gregory D Bennett; Richard Finnell; Simcha Blotnik; Meir Bialer
Stereoselective pharmacokinetic analysis of valnoctamide, a CNS-active chiral amide analogue of valproic acid, in dogs, rats, and mice.
Therapeutic drug monitoring 2000;22(5):574-81.
2000: A Volosov; Boris Yagen; Meir Bialer
Comparative stereoselective pharmacokinetic analysis of 10-hydroxycarbazepine after oral administration of its individual enantiomers and the racemic mixture to dogs.
Epilepsia 2000;41(9):1107-11.
2000: Nina Isoherranen; Michael Roeder; Stefan Soback; Boris Yagen; Volker Schurig; Meir Bialer
Enantioselective analysis of levetiracetam and its enantiomer R-alpha-ethyl-2-oxo-pyrrolidine acetamide using gas chromatography and ion trap mass spectrometric detection.
Journal of chromatography. B, Biomedical sciences and applications 2000;745(2):325-32.
2000: A Volosov; Meir Bialer; S Xiaodong; Emilio Perucca; Amnon C Sintov; Boris Yagen
Simultaneous stereoselective high-performance liquid chromatographic determination of 10-hydroxycarbazepine and its metabolite carbamazepine-10,11-trans-dihydrodiol in human urine.
Journal of chromatography. B, Biomedical sciences and applications 2000;738(2):419-25.
2000: Ofer Spiegelstein; D L Kroetz; René H Levy; Boris Yagen; S I Hurst; M Levi; Abdullah Haj-Yehia; Meir Bialer
Structure activity relationship of human microsomal epoxide hydrolase inhibition by amide and acid analogues of valproic acid.
Pharmaceutical research 2000;17(2):216-21.
2000: I Gliko-Kabir; Boris Yagen; M Baluom; Abraham Rubinstein
Phosphated crosslinked guar for colon-specific drug delivery. II. In vitro and in vivo evaluation in the rat.
Journal of controlled release : official journal of the Controlled Release Society 2000;63(1-2):129-34.
2000: I Gliko-Kabir; Boris Yagen; A Penhasi; Abraham Rubinstein
Phosphated crosslinked guar for colon-specific drug delivery. I. Preparation and physicochemical characterization.
Journal of controlled release : official journal of the Controlled Release Society 2000;63(1-2):121-7.
1999: A Volosov; S Xiaodong; Emilio Perucca; Boris Yagen; Amnon C Sintov; Meir Bialer
Enantioselective pharmacokinetics of 10-hydroxycarbazepine after oral administration of oxcarbazepine to healthy Chinese subjects.
Clinical pharmacology and therapeutics 1999;66(6):547-53.
1999: Ofer Spiegelstein; Boris Yagen; René H Levy; Richard Finnell; Gregory D Bennett; Michael Roeder; Volker Schurig; Meir Bialer
Stereoselective pharmacokinetics and pharmacodynamics of propylisopropyl acetamide, a CNS-active chiral amide analog of valproic acid.
Pharmaceutical research 1999;16(10):1582-8.
1999: Ofer Spiegelstein; Boris Yagen; Meir Bialer
Structure-pharmacokinetic-pharmacodynamic relationships of N-alkyl derivatives of the new antiepileptic drug valproyl glycinamide.
Epilepsia 1999;40(5):545-52.
1999: Ofer Spiegelstein; Meir Bialer; M Radatz; H Nau; Boris Yagen
Enantioselective synthesis and teratogenicity of propylisopropyl acetamide, a CNS-active chiral amide analogue of valproic acid.
Chirality 1999;11(8):645-50.
1998: I Gliko-Kabir; Boris Yagen; A Penhasi; Abraham Rubinstein
Low swelling, crosslinked guar and its potential use as colon-specific drug carrier.
Pharmaceutical research 1998;15(7):1019-25.
1998: M Radatz; K Ehlers; Boris Yagen; M Bialer; Heinz Nau
Valnoctamide, valpromide and valnoctic acid are much less teratogenic in mice than valproic acid.
Epilepsy research 1998;30(1):41-8.
1997: Ofer Spiegelstein; Meir Bialer; Boris Yagen
Isolation of N,N-dialkylated derivatives of valproylglycinamide from dog plasma by active charcoal adsorption and their quantification by high-performance liquid chromatography.
Journal of chromatography. B, Biomedical sciences and applications 1997;698(1-2):195-200.
1997: S Barel; Boris Yagen; V Schurig; Stefan Soback; F Pisani; E Perucca; M Bialer
Stereoselective pharmacokinetic analysis of valnoctamide in healthy subjects and in patients with epilepsy.
Clinical pharmacology and therapeutics 1997;61(4):442-9.
1997: M Levi; Boris Yagen; Meir Bialer
Pharmacokinetics and antiepileptic activity of valproyl hydroxamic acid derivatives.
Pharmaceutical research 1997;14(2):213-7.
1996: Meir Bialer; S Hadad; B Kadry; A Abdul-Hai; A Haj-Yehia; J Sterling; Y Herzig; Boris Yagen
Pharmacokinetic analysis and antiepileptic activity of tetra-methylcyclopropane analogues of valpromide.
Pharmaceutical research 1996;13(2):284-9.
1994: S Barel; Boris Yagen; Meir Bialer
Pharmacokinetic profile of conjugated verrucarol urinary metabolites in dogs.
Biopharmaceutics & drug disposition 1994;15(7):609-16.
1993: Boris Yagen; Meir Bialer
Metabolism and pharmacokinetics of T-2 toxin and related trichothecenes.
Drug metabolism reviews 1993;25(3):281-323.
1992: F Bergmann; Boris Yagen; B B Jarvis
The toxicity of macrocyclic trichothecenes administered directly into the rat brain.
Toxicon : official journal of the International Society on Toxinology 1992;30(10):1291-4.
1991: Boris Yagen; F Bergmann; S Barel; Amnon C Sintov
Metabolism of T-2 toxin by rat brain homogenate.
Biochemical pharmacology 1991;42(4):949-51.
1991: F Bergmann; Meora Feinmesser; Boris Yagen
Central effects of cycloheximide alone and of its combination with T-2 toxin.
Toxicology letters 1991;57(1):1-9.
1990: S Barel; Boris Yagen; Meir Bialer
Pharmacokinetics of the trichothecene mycotoxin verrucarol in dogs.
Journal of pharmaceutical sciences 1990;79(6):548-51.
1989: F Bergmann; R Yarom; Boris Yagen
Comparison of the toxicity of two trichothecenes applied topically to brain and liver of rats.
Toxicology letters 1989;48(1):49-56.
1989: F Bergmann; Boris Yagen
Structure-activity relationships for the direct toxic action of trichothecenes on rat brain.
Archives of toxicology 1989;63(2):155-6.
1988: Amnon C Sintov; Meir Bialer; Boris Yagen
Pharmacokinetics and protein binding of trichothecene mycotoxins, T-2 toxin and HT-2 toxin, in dogs.
Toxicon : official journal of the International Society on Toxinology 1988;26(2):153-60.
1988: F Bergmann; D Soffer; Boris Yagen
Cerebral toxicity of the trichothecene toxin T-2, of the products of its hydrolysis and of some related toxins.
Toxicon : official journal of the International Society on Toxinology 1988;26(10):923-30.
1987: Amnon C Sintov; Meir Bialer; Boris Yagen
Pharmacokinetics of T-2 tetraol, a urinary metabolite of the trichothecene mycotoxin, T-2 toxin, in dog.
Xenobiotica; the fate of foreign compounds in biological systems 1987;17(8):941-50.
1987: R Yarom; F Bergmann; Boris Yagen
Cutaneous injury by topical T-2 toxin: involvement of microvessels and mast cells.
Toxicon : official journal of the International Society on Toxinology 1987;25(2):167-74.
1986: Boris Yagen; Amnon C Sintov; Meir Bialer
New, sensitive thin-layer chromatographic-high-performance liquid chromatographic method for detection of trichothecene mycotoxins.
Journal of chromatography 1986;356(1):195-201.
1986: Amnon C Sintov; Meir Bialer; Boris Yagen
Pharmacokinetics of T-2 toxin and its metabolite HT-2 toxin, after intravenous administration in dogs.
Drug metabolism and disposition: the biological fate of chemicals 1986;14(2):250-4.
1985: F Bergmann; Boris Yagen; D Soffer
Toxic and lethal effects of T-2 toxin upon intracerebral administration to rats.
Archives of toxicology 1985;58(1):40-4.
1985: Boris Yagen; Meir Bialer; Amnon C Sintov
Gas chromatographic assay with pharmacokinetic applications for monitoring T-2 and HT-2 toxins in plasma.
Journal of chromatography 1985;343(1):67-75.