Publications relating to ETSP / ASP programs

The list of references below is a result of literature searches to identify publications that contain and acknowledged ETSP or ASP generated data or described the programs

References

Klein P, Kaminski RM, Koepp M, Löscher W. New epilepsy therapies in development. Nat Rev Drug Discov. 2024:23(9);682-708. PMID: 39039153

Erenburg N, Perucca E, Bechard J, Dube C, Weishaupt N, Sherrington R, Bialer M. Stereoselective Analysis of the Antiseizure Activity of Fenfluramine and Norfenfluramine in Mice: Is l-Norfenfluramine a Better Follow-Up Compound to Racemic-Fenfluramine? Int J Mol Sci. 2024:25(5);2522. PMID: 38473769

Melnick SM, Shin Y, Glenn KJ. Anticonvulsant effects of cenobamate in chemically and electrically induced seizure models in rodents. Heliyon. 2023:9(8);e18920. PMID: 37636350

Löscher W, White HS. Animal Models of Drug-Resistant Epilepsy as Tools for Deciphering the Cellular and Molecular Mechanisms of Pharmacoresistance and Discovering More Effective Treatments. Cells. 2023:12(9);1233. PMID: 37174633

Erenburg N, Hamed R, Shaul C, Perucca E, Bialer M. Comparative activity of the enantiomers of fenfluramine and norfenfluramine in rodent seizure models, and relationship with their concentrations in plasma and brain. Epilepsia. 2023:64(6);1673-1683. PMID: 36995363

Özdemir Z, Sari S, Karakurt A, Dalkara S. Synthesis, anticonvulsant screening, and molecular modeling studies of new arylalkylimidazole oxime ether derivatives. Drug Dev Res. 2019; 80:269–280. PMID: 30474215

Saria S, Kaynak FB, Dalkara S. Synthesis and anticonvulsant screening of 1,2,4-triazole derivatives. Pharmacological Reports 2018:70;1116–1123. PMID: 30316046

Klein BD, Jacobson CA, Metcalf CS, Smith MD, Wilcox KS, Hampson AJ, Kehne JH. Evaluation of Cannabidiol in Animal Seizure Models by the Epilepsy Therapy Screening Program (ETSP). Neurochem Res:2017; 42:1939–1948. PMID: 28478594

Kuder KJ, Łazewska D, Kaleta M, Latacz G, Kottke T, Olejarz A, Karcz T, Fruziński A, Szczepańska K, Karolak-Wojciechowska J, Stark H, Kononowicz K. Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo) piperidine derivatives as histamine H3R ligands. Bioorganic & Medicinal Chemistry. 2017; 25: 2701–2712. PMID: 28372935

Lin Z, Smith MD, Concepcion GP, Haygood MG, Olivera BM, Light A, Schmidt EW. Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products. J. Nat. Prod. 2017; 80: 2360−2370. PMID: 28745513

Waszkielewicz, A. M. et al. Design, Synthesis and Anticonvulsant Activity of Some Derivatives of Xanthone with Aminoalkanol Moieties. Chem Biol Drug Des. 2017:89;339–352. PMID: 27543433

Waszkielewicz AM, Słoczyńska K, Pękala E, Żmudzki P, Siwek A, Gryboś A, Marona H. Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties. Chemical Biology & Drug Design, 2017; 89 (3): 339-352. PMID: 27543433

Gunia-Krzyżak A, Żesławska E, Nitek W, Popiół J, Marona H. Anticonvulsant Activity of Enantiomeric N-trans-Cinnamoyl Derivatives of 2-Aminopropan-1-ols and 2-Aminobutan-1-ols. Chirality, 2016; 28 (6): 482-488. PMID: 27121961

Gunia-Krzyżak A, Żesławska E, Nitek W, Popiół J, Marona H. Anticonvulsant Activity of Enantiomeric N-trans -Cinnamoyl Derivatives of 2-Aminopropan-1-ols and 2-Aminobutan-1-ols: Anticonvulsant Activity of Enantiomeric Cinnamamide Derivatives. Chirality. 2016:28;482–488. PMID: 27121961

Kuder K, Łażewska D, Latacz G, Schwed JS, Karcz T, Stark H, Karolak-Wojciechowska J, Kieć-Kononowicz K. Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents. Bioorgan Med Chem. 2016;24:53–72. PMID: 26690914

Mawasi H, Bibi D, Bialer M. Design and comparative anticonvulsant activity assessment of CNS-active alkyl-carbamoyl imidazole derivatives. Bioorg Med Chem, 2016; 24 (18): 4246-4253. PMID: 27469980

Waszkielewicz AM, Gunia-Krzyżak A, Powroźnik B, Słoczyńska K, Pękala E, Walczak M, Bednarski M, Żesławska E, Nitek W, Marona H. Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. Bioorganic & Medicinal Chemistry, 2016; 24:1793-1810. PMID: 26988801

Coleman N, Nguyen HM, Cao Z, Brown BM, Jenkins DP, Zolkowska D, Chen Y, Tanaka BS, Goldin AL, Rogawski MA, Pessah IN, Wulff H. The riluzole derivative 2-amino-6-trifluoromethylthio-benzothiazole (SKA-19), a mixed KCa2 activator and NaV blocker, is a potent novel anticonvulsant. Neurotherapeutics, 2015; 12 (1): 234-249. PMID: 25256961

Kamiński K, Wiklik B, Obniska J. Synthesis and anticonvulsant activity of new N-phenyl-2- (4-phenylpiperazin-1-yl)acetamide derivatives. Med Chem Res. 2015:24;3047–3061. PMID: 26167103

Park KD, Yang X, Dustrude ET, Wang Y, Ripsch MS, White FA, Khanna R, Kohn H. Chimeric Agents Derived from the Functionalized Amino Acid, Lacosamide, and the α Aminoamide, Safinamide: Evaluation of Their Inhibitory Actions on Voltage-Gated Sodium Channels, and Antiseizure and Antinociception Activities and Comparison with Lacosamide and Safinamide. ACS Chem. Neurosci. 2015:6;316−330. PMID: 25418676

Strupińska M, Rostafińska-Suchar G, Pirianowicz-Chaber E, Grabczuk M, Józwenko M, Kowalczyk H, Szuba J, Wójcicka M, Chen T, Mazurek AP. Synthesis and study of halogenated benzylamides of some isocyclic and heterocyclic acids as potential anticonvulsants. Acta Pol. Pharm. Drug Research. 2015; 72: 489-496. PMID: 26642657

Torregrosa R, Yang X, Dustrude ET, Cummins TR, Khanna R, Kohn H. Chimeric Derivatives of Functionalized Amino Acids and α-Aminoamides: Compounds with Anticonvulsant Activity in Seizure Models and Inhibitory Actions on Central, Peripheral, and Cardiac Isoforms of Voltage-gated Sodium Channels. Bioorg. Med Chem. 2015:23;3655–3666. PMID: 25922183

Dawidowski M, Lewandowski W, Turło J. Synthesis of New Perhydropyrrolo[1,2-a]pyrazine Derivatives and Their Evaluation in Animal Models of Epilepsy. Molecules 2014:19;15955-15981. PMID: 25295751

Lee H, Park KD, Torregrosa R, Yang X, Dustrude ET, Wang Y, Wilson SM, Barbosa C, Xiao Y, Cummins TR, Khanna R, Kohn H. Substituted N (Biphenyl-4′-yl)methyl (R) 2-Acetamido-3- methoxypropionamides: Potent Anticonvulsants That Affect Frequency (Use) Dependence and Slow Inactivation of Sodium Channels. J. Med. Chem. 2014:57;6165−6182. PMID: 25004277

Dawidowski M, Wilczek M, Kubica K, Skolmowski M, Turło J. Structure–activity relationships of the aromatic site in novel anticonvulsant pyrrolo[1,2-a]pyrazine derivatives. Bioorganic & Medicinal Chemistry Letters 2013:23;6106–6110. PMID: 24095092

White HS, Alex AB, Pollock A, Hen N, Shekh-Ahmad T, Wilcox KS, McDonough JH, Stables JP, Kaufmann D, Yagen B, Bialer M. 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;134–146. PMID: 22150444

Tripathi L, Singh R, Stables JP. Design & synthesis of N′-[substituted] pyridine-4-carbohydrazides as potential anticonvulsant agents. Eur J Med Chem. 2011:46;509–518. PMID: 21167624

Obniska J, Kaminski K, Skrzynska D, Pichor J. Synthesis and anticonvulsant activity of new N-[(4-arylpiperazin-1-yl)-alkyl] derivatives of 3-phenyl-pyrrolidine-2,5-dione. Eur J Med Chem. 2009:44;2224–2233. PMID: 18603334

Shimshoni JA, Bialer M, Wlodarczyk B, Finnell RH, Yagen B. Potent anticonvulsant urea derivatives of constitutional isomers of valproic acid. J Med Chem. 2007:50;6419–6427. PMID: 17994680

Obniska J, Dzierzawska-Majewska A, Zagorska A, Zajdel P, Karolak-Wojciechowska J. Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I. Farmaco. 2005:60;529-539. PMID: 15950973

Paruszewski R, Strupińska M, Stables JP, Swiader M, Czuczwar S, Kleinrok Z, Turski W. Amino Acid Derivatives with Anticonvulsant Activity. Chem Pharm Bull (Tokyo). 2001:49;629–631. PMID: 11383620

Ucar H, Van derpoorten K, Cacciaguerra S, Spampinato S, Stables JP, Depovere P, Isa M, Masereel B, Delarge J, Poupaert JH. Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. J Med Chem. 1998:41;1138-1145. PMID: 9544213

Carson JR, Carmosin RJ, Pitis PM, Vaught JL, Almond HR, Stables JP, Wolf HH, Swinyard EA, White HS. Aroyl(aminoacyl)pyrroles, a New Class of Anticonvulsant Agents. J. Med. Chem. 1997; 40: 1578–1584. PMID: 9171868

Dimmock JR, Puthucode RN, Smith JM, Hetherington M, Quail JW, Pugazhenthi U, Lechler T, Stables JP. (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. J Med Chem. 1996:39;3984–3997. PMID: 8831764