New Phenylglycinamide Derivatives with Hybrid Structure as Candidates for New Broad-Spectrum Anticonvulsants

Autor: Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Gniewomir Latacz, Bartłomiej Szulczyk, Katarzyna Socała, Dorota Nieoczym, Piotr Wlaź, Cameron S. Metcalf, Karen Wilcox, Rafał M. Kamiński, Krzysztof Kamiński

Publikováno v: Cells, Vol 11, Iss 12, p 1862 (2022)

In the present study, a focused combinatorial chemistry approach was applied to merge structural fragments of well-known TRPV1 antagonists with a potent anticonvulsant lead compound, KA-104, that was previously discovered by our group. Consequently,

Externí odkaz: https://doaj.org/article/9d34a801f4aa4feab4747cefcea04a31

KA‐104, a new multitargeted anticonvulsant with potent antinociceptive activity in preclinical models

Autor: Michał Abram, Kamil Kuś, Szczepan Mogilski, Karolina Matyjaszczyk, Krzysztof Kamiński, Anna Rapacz, Bartłomiej Szulczyk, Maria Walczak, Rafał M. Kamiński, Gniewomir Latacz

Publikováno v: Epilepsia. 61:2119-2128

Objective The main objective of the present work was to assess the utility of KA-104 as potential therapy for drug-resistant seizures and neuropathic pain, and to characterize its druglike properties in a series of absorption, distribution, metabolis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::55f18909a3f37e2768c466c3216b2569
https://doi.org/10.1111/epi.16669

Identification of New Compounds with Anticonvulsant and Antinociceptive Properties in a Group of 3-substituted (2,5-dioxo-pyrrolidin-1-yl)(phenyl)-Acetamides

Autor: Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Bartłomiej Szulczyk, Małgorzata Szafarz, Katarzyna Socała, Dorota Nieoczym, Elżbieta Wyska, Piotr Wlaź, Rafał M. Kamiński, Krzysztof Kamiński

Publikováno v: International Journal of Molecular Sciences
International Journal of Molecular Sciences; Volume 22; Issue 23; Pages: 13092
International Journal of Molecular Sciences, Vol 22, Iss 13092, p 13092 (2021)

We report herein a series of water-soluble analogues of previously described anticonvulsants and their detailed in vivo and in vitro characterization. The majority of these compounds demonstrated broad-spectrum anticonvulsant properties in animal sei

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03a8ea4fd73cd7e78348534ade4042ae
http://europepmc.org/articles/PMC8658016

Asymmetric synthesis and in vivo/in vitro characterization of new hybrid anticonvulsants derived from (2,5-dioxopyrrolidin-1-yl)phenylacetamides

Autor: Marta Struga, Michał Abram, Rafał M. Kamiński, Dagmara Otto-Ślusarczyk, Justyna Kalinowska-Tłuścik, Gniewomir Latacz, Bartłomiej Szulczyk, Anna Rapacz, Krzysztof Kamiński

Publikováno v: Bioorganic chemistry. 109

In the current studies we carried out an optimized multistep asymmetric synthesis of R-enantiomers (eutomers) for a previously identified series of racemic hybrid anticonvulsants. The spatial structure of selected enantiomers was solved by the use of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6d654db5c33ddfe98dfc6b51b25251a9
https://pubmed.ncbi.nlm.nih.gov/33647745

Multitargeted Compounds Derived from (2,5-Dioxopyrrolidin-1-yl)(phenyl)-Acetamides as Candidates for Effective Anticonvulsant and Antinociceptive Agents

Autor: Szczepan Mogilski, Annamaria Lubelska, Rafał M. Kamiński, Krzysztof Kamiński, Gniewomir Latacz, Michał Abram, Anna Rapacz

Publikováno v: ACS chemical neuroscience. 11(13)

We developed a focused set of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant and antinociceptive properties. These hybrid compounds demonstrated broad-spectrum protective activity in a range of mouse models, such as the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37dc0cdb4c2acc51babb4e48281d0654
https://pubmed.ncbi.nlm.nih.gov/32479058