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-Reference-Cited by-同舟云学术

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

Published:2022-08-19 Issue:17 Volume:65 Page:11703-11725
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Abram Michał¹^ORCID,Jakubiec Marcin¹,Reeb Katelyn²,Cheng Mary Hongying³^ORCID,Gedschold Robin⁴,Rapacz Anna⁵,Mogilski Szczepan⁵,Socała Katarzyna⁶^ORCID,Nieoczym Dorota⁶,Szafarz Małgorzata⁷,Latacz Gniewomir⁸,Szulczyk Bartłomiej⁹,Kalinowska-Tłuścik Justyna¹⁰^ORCID,Gawel Kinga¹¹,Esguerra Camila V.¹²,Wyska Elżbieta⁷^ORCID,Müller Christa E.⁴^ORCID,Bahar Ivet³^ORCID,Fontana Andréia C. K.²^ORCID,Wlaź Piotr⁶,Kamiński Rafał M.¹,Kamiński Krzysztof¹^ORCID

Affiliation:

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688Krakow, Poland

2. Department of Pharmacology and Physiology, Drexel University College of Medicine, Philadelphia, Pennsylvania19102, United States

3. Department of Computational and Systems Biology, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania15213, United States

4. PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, Rheinische Friedrich-Wilhelms-Universität Bonn, An der Immenburg 4, D-53121Bonn, Germany

5. Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688Krakow, Poland

6. Department of Animal Physiology and Pharmacology, Institute of Biological Sciences, Faculty of Biology and Biotechnology, Maria Curie-Skłodowska University, Akademicka 19, 20-033Lublin, Poland

7. Department of Pharmacokinetics and Physical Pharmacy, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688Krakow, Poland

8. Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688Krakow, Poland

9. Department of Pharmacodynamics, Centre for Preclinical Research and Technology, Medical University of Warsaw, Banacha 1B, 02-097Warsaw, Poland

10. Department of Crystal Chemistry and Crystal Physics, Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387Krakow, Poland

11. Department of Experimental and Clinical Pharmacology, Medical University of Lublin, Jaczewskiego 8B, 20-090Lublin, Poland

12. Chemical Neuroscience Group, Centre for Molecular Medicine Norway, University of Oslo, Gaustadalléen 21, Forskningsparken, 0349Oslo, Norway

Funder

Narodowe Centrum Nauki

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c00534

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