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Researchers
  • Prof.  Boris Yagen
Prof Boris Yagen
 
Research Projects
  

        ·       Structure activity relationship studies of CNS active valproylamides, glycine and taurine

        ·       Chemistry and toxicology of antiepileptic drugs
 
 
 
Journal Articles
 
Gliko-Kabir, I., Yagen, B., Penhasi, A. and Rubinstein, A. Phosphated crosslinked guar for colon-secific drug delivery: I. Preparation and physical and   chemical characterization. J. Contr. Rel.,. 63: 121-127 (2000).
 
O. Spiegelstein, D.L. Kroetz, R.H. Levy, B. Yagen, S.I. Hurst, M. Levi, A. Haj-Yehia and M. Bialer Structure activity relationships of human microsomal epoxide hydroalse inhibition by amide and acid analogues of valproic acid. Pharm. Res., 17:216-221 (2000).
 
Gliko-Kabir, I., Yagen, B., Baluom, M. and Rubinstein, A.Phosphated crosslinked guar for colon-specific drug delivery: II. In vitro and in vivo evaluation.
J.Contr. Rel., 63: 129-134, (2000).
 
N. Isoherranen, B. Yagen, S. Soback, M. Roeder, V. Schurig and M. Bialer: Pharmacokinetic analysis of levetiracetam and its enantiomer R-alpha-ethyl-2-oxo-pyrrolidine acetamide in dogs. Epilepsia 42:825-830 (2001).
 
N. Isoherranen, H.S. White, R.H. Finnell, B. Yagen, J.H Woodhead, G.D. Bennett, K.S. Wilcox, M.E. Barton and M Bialer: Anticonvulsant profile and teratogenicity of N-methyl tetramethylcyclopropyl carboxamide: A new antiepileptic drug. Epilepsia 43:115-126 (2002).
 
N. Isoherranen, B. Yagen, O. Spiegelstein, A. Steinman, R.H. Finnell and M. Bialer: Gas-chromatographic determination of novel valproyltaurinamide derivatives in mouse and dog plasma samples. J. Chromatog. B., 788:125-136 (2003).
 
N. Isoherranen, B. Yagen, S. Blotnik, O. Spiegelstein, K.S. Wilcox, J.H. Woodhead, R.H. Finnell, H.S. White and M. Bialer: Characterization of the anticonvulsant activity and pharmacokinetics of propylisopropyl acetamide and its enantiomers. Br. J. Pharmacol. 138:602-613 (2003).
 
N. Isoherranen, H.S. White, B.D. Klein, M. Roeder, B. Yagen, J.H. Woodhead, V. Schurig and M. Bialer: Pharmacokinetic-pharmacodynamic relationships of 2S,3S-valnoctamide and its stereoisomer 2R,3S-valnoctamide in animal models for epilepsy. Pharm. Res.20:1293-1301 (2003).
 
N. Isoherranen, B. Yagen, O. Spiegelstein, R.H. Finnell, M. Merriweather, J.H. Woodhead, N. Wlodarczxyk, H.S. White and M. Bialer: Anticonvulsant activity, teratogenicity and pharmacokinetics of novel valproyltaurinamide derivatives in mice. Brit. J. Pharmacol.139:755-764 (2003).
 
N. Isoherranen, B. Yagen and M. Bialer: New CNS-active drugs which are second generation valproic acid: Can they lead to the development of the magic bullet? Curr. Opin. Neurol. 16:203-211 (2003).
 
N. Isoherranen, O. Spiegelstein, M. Bialer, J. Zhang, M. Merriweather, B. Yagen, M. Roeder, A.A. Tripplett, V. Schurig and R.H. Finnell: Developmental outcome of levetiracetam, its major acid metabolite in humans (R)-α-ethyl-oxo-pyrrolidone 2-pyrrolidinone N-butyric acid and its enantiomer in a mouse model of antiepileptic drug teratogenicity. Epilepsia 44:1280-1288 (2003).
 
N. Isoherranen, R.H. Levy, B. Yagen, J.H. Woodhead, H.S. White and M. Bialer: Metabolism of a new antiepileptic drug, N-methyl cyclopropane carboxamide, and anticonvulsant activity of its metabolites. Epilepsy Res.58:1-12 (2004).
 
S. Eyal, B. Yagen, E. Sobol, Y. Altschuler, M. Shmuel and M. Bialer: The activity of antiepileptic drugs as histone deacetylase inhibitors. Epilepsia 45:737-744 (2004).
 
E. Sobol. M. Bialer and B. Yagen. Tetramethylcyclopropyl analogue of a leading antiepileptic drug-valproic acid. Synthesis and evaluation of its amide derivatives. J. Med. Chem., 47:4316-4326 (2004).
 
S. Eyal, B. Yagen, J. Shimshoni, and M. Bialer. Histone deacetylase inhibition and tumor cells cytotoxicity by CNS-active VPA constitutional isomers and derivatives. Biochem. Pharmacol.69:1501-1508 (2005).
 
I. Winkler, S. Blotnik, J. Shimshoni, B. Yagen, M. Devor and M. Bialer. Efficacy of antiepileptic isomers of valproic acid and valpromide in a rat model of neuropathic pain. Brit. J. Pharmacol., 146:198-2008 (2005).
 
I. Winkler, E. Sobol, B. Yagen, A. Steinman, M. Devor and M. Bialer. Efficacy of antiepileptic tetramethylcyclopropyl analogs of valproic acid amides in a rat model for neuropathic pain. Neuropharmacology, 49:1110-1120 (2005).
 
E. Sobol, B. Yagen, I. Winkler, M. Britzi, D. Gibson and M. Bialer. Pharmacokinetics and metabolism of a new potent anticonvulsant agent, 2,2,3,3-tetramethylcyclopropylcarbonylurea in rats. Drug Metab. Disposit, 33:1538-1546 (2005).
 
A. Okada, Y. Onishi, Y. Aoki, K. B. Yagen, E. Sobol, M. Bialer and M. Fujiwara: Teratology studies of derivatives of tetramethylcyclopropyl amide analogues of valproic acid in mice. Birth Defect. Res. (Part B) 77:227-233 (2006).
 
S. Eyal, J. G. Lamb, M. Smith-Yockman, B. Yagen, E. Fibach, Y. Altschuler, H. S. White and M. Bialer: The antiepileptic and chemotherapeutic agent valproic acid induces P-glycoprotein in human tumor cell lines and in rat liver. Brit. J. Pharmacol. 149:250-260 (2006).
 
E. Sobol, B. Yagen, H. S. White, K. S. Wilcox, J. G. Lamb, O. Pappo, B. Wlodarczyk, R.H. Finnell and M. Bialer. Preclinical evaluation of 2,2,3,3-tetramethylcyclopropanecarbonylurea, a novel second generation to valproic acid, antiepileptic drug. Neuropharmacology 51:933-946 (2006).
 
E. Sobol, B. Yagen, J. G. Lamb, H. S. White, B. Wlodarczyk, R.H. Finnell and M. Bialer. Anticonvulsant activity, mutagenicity and pharmacokinetics of a new potent antiepileptic drug, N-methoxy-2,2,3,3-tetramethylcyclopropanecarbxamide. Epilepsy Res. 73:75-84 (2007).
 
M. Bialer, B. Yagen. Valproic acid – Second generation. Neurotherapeutics, 4:130-137 (2007).
 
J. Shimshoni, E. C. Dalton, A. Jenkins, S. Eyal, K. Ewen, R. S. B. Williams, N. Pessah, B. Yagen, J. A. Harwood and M. Bialer. The effect of CNS-active valproic acid constitutional isomers, cyclopropyl analogues and amide derivatives on neuronal growth cone behavior. Mol Pharmacol., 71:884-892 (2007).
 
M. Bialer, B. Yagen. Valproic acid – Second generation. Neurotherapeutics, 4:130-137 (2007).
 
J. Shimshoni, E. C. Dalton, A. Jenkins, S. Eyal, K. Ewen, R. S. B. Williams, N. Pessah, B. Yagen, J. A. Harwood and M. Bialer. The effect of CNS-active valproic acid constitutional isomers, cyclopropyl analogues and amide derivatives on neuronal growth cone behavior. Mol Pharmacol., 71:884-892 (2007).
 
J. A.  Shimishoni, B. Bialer, B. Wlodarczyk, R. H. Finnell and B. Yagen. Potent anticonvulsant urea derivatives of constitutional isomers of valproic acid. J. Med. Chem. 50: 6419- 6427 (2007).
 
D. Kaufmann, B. Yagen, A. Minert, M. Tal, M. Devor and M. Bialer. Evaluation of the enantioselective antiallodynic profile and pharmacokinetics of propylisopropylacetamide, a chiral isomer of valproic acid amide. Neuropharmacology 54:699-707 (2008).
 
J. Shimishoni, M Bialer and B. Yagen. Synthesis and anticonvulsant activity of new tetramethylcyclpopropylcarboaxamide aromatic derivatives. Bioorg. Med. Chem. 16:6297-6305 (2008).
 
J A. Shimishoni, B. Yagen, N. Pessah, B. Wlodarczyk, R. H. Finnell and M. Bialer. Anticonvulsant profile and teratogenicity of 3,3-dimethylbutanoylurea: A potential for a second generation drug to valproic acid. Epilepsia, (2008) in press.
 
A. Okada, Y. Onishi, B. Yagen, J. A. Shimshoni, D. A Kaufamnn, M. Bialer and M. Fujiwara: Tetramethylcyclopropyl analogue of the leading antiepileptic drug, valproic acid. Evaluation of the teratogenic effects of its amide derivatives in NMRI mice. Birth Defects Res. Part B Dev. Reprod. Toxicol. (2008) In press
 
 
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Collaborations 
NIH Epilepsy Branch.
 
Prof. Rene H. Levy, Univ. of Washington, Seattle, USA.
 
Prof. H. Steve White, Univ of Utah, USA.
 
Prof. Richard Finell, Texas A&M Univ., USA.
 
Prof. Meir Bialer, The Hebrew Unievraity of Jerusalem.
 
Prof. Marshal Devor, The Hebrew University of Jerusalem.
 
 
Patents  

M. Bialer, O. Spiegelstein and B. Yagen. Propylisopropyl acetic acid and propylisopropyl acetamide steroisomers, a method for their synthesis and pharmaceutical compositions containing them. U.S. Patent Applic. Ser. No. 09/673,296. Filing 13.10.2000. 

M. Bialer, N. Isoherranen and B. Yagen. Derivatives of valproyl taurinamide, method of making and use thereof as anticonvulsant and CNS active agents. U.S. Prov. Pat. Applic. Ser. No. 60/300,416. Filing 26.6.2001. Int. Applic. No. PCT/IL01/00175. Filing 5.3.2002. 

M. Bialer, N. Isoherranen and B. Yagen. Derivatives and pharmaceutical composition of N-Hydroxymethyl Tetramethylcyclopropyl-Carboxamide having anti-epileptic, neurological and CNS activity, and method for their preparation. IL Pat. No. 147953. Filing 1.2.2002. Int. Applic. No. PCT/IL02/0150. Filing 27.12.2002. 

M. Bialer, B. Yagen and E. Sobol. New Amide derivatives of 2,2,3,3-tetramethylcyclopropane carboxylic acid, a method their synthesis and pharmaceutical compositions containing them. IL patent application No. 154694. Filing date: 28 February 2003, and IL patent application No.157751. Filing date: 4 September 2003. 

M. Bialer, B. Yagen, H. Pinchas Belmaker, G. Agam and G. Shaltiel. Use of 2,2,3,3, tetramethylcyclopropane carboxylic acid derivatives for treating psychiatric disorders. IL Patent Application No. 156203. Filing Date: 29 May 2003. 

M. Bialer, B. Yagen, S. Eyal and Y. Altschuler. Topiramate compositions useful for the treatment of cancer. IL Patent Application No.156888. Filing Date: 29 June 2003. 

I. Winkler, M. Bialer, B. Yagen and M. Devor. Compounds useful for treating neurological disorders. US Provisional Patent Application Serial No.60/490,273. Filing Date: 28 July 2003. 

M. Bialer, B. Yagen and S. Eyal. Use of valproyl hydroxamic acid as an antineoplastic agent. IL Patent Application No. 162263. Filing Date: 31 May 2004. 

 

 

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