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Publications in the selection

34 hits

Bibliografisk träff 2022-08-19

Discovery of (R)-N-Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS-1], a Novel Orally Bioavailable EAAT2 Modulator with Drug-like Properties and Potent Antiseizure Activity In Vivo.

Abram M, Jakubiec M, Reeb K, Cheng MH, Gedschold R, Rapacz A, Mogilski S, Socała K, Nieoczym D, Szafarz M, Latacz G, Szulczyk B, Kalinowska-Tłuścik J, Gawel K, Esguerra CV, Wyska E, Müller CE, Bahar I, Fontana ACK, Wlaź P, Kamiński RM, Kamiński K.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.2c00534

Bibliografisk träff 2022-08-01

Inhibition of NaV1.7: the possibility of ideal analgesics.

Kitano Y, Shinozuka T.

RSC Med Chem · review-article; review; journal article · DOI 10.1039/d2md00081d

Bibliografisk träff 2020-06-07

Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.

Pańczyk K, Rapacz A, Furgała-Wojas A, Sałat K, Koczurkiewicz-Adamczyk P, Łucjanek M, Skiba-Kurek I, Karczewska E, Sowa A, Żelaszczyk D, Siwek A, Popiół J, Pękala E, Marona H, Waszkielewicz A.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127325

Bibliografisk träff 2019-09-06

Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Bai Y, He X, Bai Y, Sun Y, Zhao Z, Chen X, Li B, Xie J, Li Y, Jia P, Meng X, Zhao Y, Ding Y, Xiao C, Wang S, Yu J, Liao S, Zhang Y, Zhu Z, Zhang Q, Zhao Y, Qin F, Zhang Y, Wei X, Zeng M, Liang J, Cuan Y, Shan G, Fan TP, Wu B, Zheng X.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.111650

Bibliografisk träff 2017-10-04

Multifunctional Hybrid Compounds Derived from 2-(2,5-Dioxopyrrolidin-1-yl)-3-methoxypropanamides with Anticonvulsant and Antinociceptive Properties.

Abram M, Zagaja M, Mogilski S, Andres-Mach M, Latacz G, Baś S, Łuszczki JJ, Kieć-Kononowicz K, Kamiński K.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.7b01114

Bibliografisk träff 2017-04-28

The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.

Pryde DC, Swain NA, Stupple PA, West CW, Marron B, Markworth CJ, Printzenhoff D, Lin Z, Cox PJ, Suzuki R, McMurray S, Waldron GJ, Payne CE, Warmus JS, Chapman ML.

Medchemcomm · research-article; journal article · DOI 10.1039/c7md00131b

Bibliografisk träff 2017-02-04

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and its 3-methyl-, 3-isopropyl, and 3-benzhydryl analogs.

Rybka S, Obniska J, Rapacz A, Filipek B, Żmudzki P.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.02.002

Bibliografisk träff 2016-11-11

Design, synthesis and anticonvulsant-analgesic activity of new N-[(phenoxy)alkyl]- and N-[(phenoxy)ethoxyethyl]aminoalkanols.

Rapacz A, Waszkielewicz AM, Pańczyk K, Pytka K, Koczurkiewicz P, Piska K, Pękala E, Budziszewska B, Starek-Świechowicz B, Marona H.

Medchemcomm · research-article; journal article · DOI 10.1039/c6md00537c

Bibliografisk träff 2016-05-02

Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides.

Kamiński K, Rapacz A, Filipek B, Obniska J.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2016.04.066

Bibliografisk träff 2016-03-21

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from 3-(1-phenylethyl)- and 3-benzyl-pyrrolidine-2,5-dione.

Rybka S, Obniska J, Rapacz A, Furgała A, Filipek B, Żmudzki P.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2016.03.075

Bibliografisk träff 2016-03-03

DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.

Chen M, Suzuki A, Thakkar S, Yu K, Hu C, Tong W.

Drug Discov Today · review; journal article · DOI 10.1016/j.drudis.2016.02.015

Bibliografisk träff 2015-12-18

New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones.

Kamiński K, Zagaja M, Rapacz A, Łuszczki JJ, Andres-Mach M, Abram M, Obniska J.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.12.027

Bibliografisk träff 2015-06-23

Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides.

Kamiński K, Zagaja M, Łuszczki JJ, Rapacz A, Andres-Mach M, Latacz G, Kieć-Kononowicz K.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b00578

Bibliografisk träff 2015-04-11

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.

Torregrosa R, Yang XF, Dustrude ET, Cummins TR, Khanna R, Kohn H.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2015.04.014

Bibliografisk träff 2015-03-21

Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives.

Kamiński K, Rapacz A, Łuszczki JJ, Latacz G, Obniska J, Kieć-Kononowicz K, Filipek B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.03.038

Bibliografisk träff 2014-08-04

Novel fluorinated pyrrolo[1,2-a]pyrazine-2,6-dione derivatives: synthesis and anticonvulsant evaluation in animal models of epilepsy.

Dawidowski M, Chońska J, Mika W, Turło J.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2014.07.042

Bibliografisk träff 2014-07-31

Prediction of Thorough QT study results using action potential simulations based on ion channel screens.

Mirams GR, Davies MR, Brough SJ, Bridgland-Taylor MH, Cui Y, Gavaghan DJ, Abi-Gerges N.

J Pharmacol Toxicol Methods · research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.vascn.2014.07.002

Bibliografisk träff 2013-11-01

Benzyloxybenzylammonium chlorides: Simple amine salts that display anticonvulsant activity.

Lee H, Gold AS, Yang XF, Khanna R, Kohn H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2013.10.031

Bibliografisk träff 2013-08-16

A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

Morgan RE, van Staden CJ, Chen Y, Kalyanaraman N, Kalanzi J, Dunn RT, Afshari CA, Hamadeh HK.

Toxicol Sci · journal article · DOI 10.1093/toxsci/kft176

Bibliografisk träff 2013-07-03

(Biphenyl-4-yl)methylammonium chlorides: potent anticonvulsants that modulate Na+ currents.

Lee H, Park KD, Yang XF, Dustrude ET, Wilson SM, Khanna R, Kohn H.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm4007092

Bibliografisk träff 2012-11-29

Ion channels as therapeutic targets: a drug discovery perspective.

Bagal SK, Brown AD, Cox PJ, Omoto K, Owen RM, Pryde DC, Sidders B, Skerratt SE, Stevens EB, Storer RI, Swain NA.

J Med Chem · review; journal article · DOI 10.1021/jm3011433

Bibliografisk träff 2012-04-11

Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides.

Baruah PK, Dinsmore J, King AM, Salomé C, De Ryck M, Kaminski R, Provins L, Kohn H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2012.04.002

Bibliografisk träff 2011-09-13

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.

King AM, Salomé C, Salomé-Grosjean E, De Ryck M, Kaminski R, Valade A, Stables JP, Kohn H.

J Med Chem · research support, non-u.s. gov't; journal article; research support, n.i.h., extramural · DOI 10.1021/jm200759t

Bibliografisk träff 2011-09-13

Defining the structural parameters that confer anticonvulsant activity by the site-by-site modification of (R)-N'-benzyl 2-amino-3-methylbutanamide.

King AM, De Ryck M, Kaminski R, Valade A, Stables JP, Kohn H.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm200760a

Bibliografisk träff 2011-07-22

Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: perhydropyrrole[1,2-a]pyrazines.

Dawidowski M, Herold F, Chodkowski A, Kleps J, Szulczyk P, Wilczek M.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2011.07.027

Bibliografisk träff 2011-06-15

Primary amino acid derivatives: compounds with anticonvulsant and neuropathic pain protection activities.

King AM, Salomé C, Dinsmore J, Salomé-Grosjean E, De Ryck M, Kaminski R, Valade A, Kohn H.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm2004305

Bibliografisk träff 2010-08-01

The structure-activity relationship of the 3-oxy site in the anticonvulsant (R)-N-benzyl 2-acetamido-3-methoxypropionamide.

Morieux P, Salomé C, Park KD, Stables JP, Kohn H.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm100508m

Bibliografisk träff 2010-05-01

Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.

Salomé C, Salomé-Grosjean E, Stables JP, Kohn H.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm100185c

Bibliografisk träff 2010-02-01

Synthesis and anticonvulsant activities of (R)-N-(4'-substituted)benzyl 2-acetamido-3-methoxypropionamides.

Salomé C, Salomé-Grosjean E, Park KD, Morieux P, Swendiman R, DeMarco E, Stables JP, Kohn H.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm901563p

Bibliografisk träff 2010-01-01

The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors.

Temperini C, Innocenti A, Scozzafava A, Parkkila S, Supuran CT.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm901524f

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Publications in the selection

Discovery of (<i>R</i>)-<i>N</i>-Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [<b>(<i>R</i>)-AS-1</b>], a Novel Orally Bioavailable EAAT2 Modulator with Drug-like Properties and Potent Antiseizure Activity <i>In Vivo</i>.

Inhibition of Na<sub>V</sub>1.7: the possibility of ideal analgesics.

Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.

Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Multifunctional Hybrid Compounds Derived from 2-(2,5-Dioxopyrrolidin-1-yl)-3-methoxypropanamides with Anticonvulsant and Antinociceptive Properties.

The discovery of a potent Na<sub>v</sub>1.3 inhibitor with good oral pharmacokinetics.

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and its 3-methyl-, 3-isopropyl, and 3-benzhydryl analogs.

Design, synthesis and anticonvulsant-analgesic activity of new <i>N</i>-[(phenoxy)alkyl]- and <i>N</i>-[(phenoxy)ethoxyethyl]aminoalkanols.

Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides.

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from 3-(1-phenylethyl)- and 3-benzyl-pyrrolidine-2,5-dione.

DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.

New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones.

Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides.

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.

Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives.

Novel fluorinated pyrrolo[1,2-a]pyrazine-2,6-dione derivatives: synthesis and anticonvulsant evaluation in animal models of epilepsy.

Prediction of Thorough QT study results using action potential simulations based on ion channel screens.

Benzyloxybenzylammonium chlorides: Simple amine salts that display anticonvulsant activity.

A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

(Biphenyl-4-yl)methylammonium chlorides: potent anticonvulsants that modulate Na+ currents.

Ion channels as therapeutic targets: a drug discovery perspective.

Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides.

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.

Defining the structural parameters that confer anticonvulsant activity by the site-by-site modification of (R)-N'-benzyl 2-amino-3-methylbutanamide.

Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: perhydropyrrole[1,2-a]pyrazines.

Primary amino acid derivatives: compounds with anticonvulsant and neuropathic pain protection activities.

The structure-activity relationship of the 3-oxy site in the anticonvulsant (R)-N-benzyl 2-acetamido-3-methoxypropionamide.

Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.

Synthesis and anticonvulsant activities of (R)-N-(4'-substituted)benzyl 2-acetamido-3-methoxypropionamides.

The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors.