Research progress in biological activities of succinimide derivatives

Z Zhao, J Yue, X Ji, M Nian, K Kang, H Qiao… - Bioorganic …, 2021 - Elsevier
Succinimides are well recognized heterocyclic compounds in drug discovery which produce
diverse therapeutically related applications in pharmacological practices. Researches in …

Advances in epilepsy: mechanisms, clinical trials, and drug therapies

T Hu, J Zhang, J Wang, L Sha, Y Xia… - Journal of medicinal …, 2023 - ACS Publications
Epilepsy is a common disease of the nervous system characterized by transient brain
dysfunction caused by an abnormal electrical discharge from the brain neurons. The …

Chirality as an important factor for the development of new antiepileptic drugs

M Abram, M Jakubiec, K Kamiński - ChemMedChem, 2019 - Wiley Online Library
In recent years, chiral molecules (especially enantiomers) have occupied a significant place
in pharmaceutical industry and have played a prominent role in the development of new …

Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain

C Liu, R Miao, F Raza, H Qian, X Tian - European Journal of Medicinal …, 2023 - Elsevier
Diabetic neuropathic pain (DNP) is a common, complex, and severe complication of
diabetes. It can lead to increased mortality, lower-limb amputations, and distressing …

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 …

M Abram, M Jakubiec, K Reeb, MH Cheng… - Journal of medicinal …, 2022 - ACS Publications
(R)-7 [(R)-AS-1] showed broad-spectrum antiseizure activity across in vivo mouse seizure
models: maximal electroshock (MES), 6 Hz (32/44 mA), acute pentylenetetrazol (PTZ), and …

KA-11, a novel pyrrolidine-2, 5-dione derived broad-spectrum anticonvulsant: Its antiepileptogenic, antinociceptive properties and in vitro characterization

K Socała, S Mogilski, M Pieróg… - ACS chemical …, 2018 - ACS Publications
Recently, compound KA-11 was identified as a promising candidate for a new broad-
spectrum anticonvulsant. This compound revealed wide protective activity across the most …

An update on the novel methods for the discovery of antiseizure and antiepileptogenic medications: where are we in 2024?

A Talevi, C Bellera - Expert Opinion on Drug Discovery, 2024 - Taylor & Francis
Introduction Despite the availability of around 30 antiseizure medications, 1/3 of patients
with epilepsy fail to become seizure-free upon pharmacological treatment. Available …

Multitargeted compounds derived from (2, 5-dioxopyrrolidin-1-yl)(phenyl)-acetamides as candidates for effective anticonvulsant and antinociceptive agents

M Abram, A Rapacz, S Mogilski, G Latacz… - ACS Chemical …, 2020 - ACS Publications
We developed a focused set of original hybrid pyrrolidine-2, 5-dione derivatives with potent
anticonvulsant and antinociceptive properties. These hybrid compounds demonstrated …

Synthesis, anticonvulsant and antinociceptive activity of new hybrid compounds: derivatives of 3-(3-methylthiophen-2-yl)-pyrrolidine-2, 5-dione

M Góra, A Czopek, A Rapacz, A Dziubina… - International Journal of …, 2020 - mdpi.com
The present study aimed to design and synthesize a new series of hybrid compounds with
pyrrolidine-2, 5-dione and thiophene rings in the structure as potential anticonvulsant and …

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

M Abram, M Jakubiec, A Rapacz, S Mogilski… - International journal of …, 2021 - mdpi.com
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 …