Unlocking the potential of higher-molecular-weight 5-HT

ADMET properties Docking G protein-coupled receptors Gene expression assay MTS assay Molecular modelling Serotonin receptor 5-HT(7) in vitro experiments

Journal

Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703

Informations de publication

Date de publication:
24 Jul 2024
Historique:
received: 20 05 2024
revised: 10 07 2024
accepted: 22 07 2024
medline: 31 7 2024
pubmed: 31 7 2024
entrez: 30 7 2024
Statut: aheadofprint

Résumé

An increasing number of drugs introduced to the market and numerous repositories of compounds with confirmed activity have posed the need to revalidate the state-of-the-art rules that determine the ranges of properties the compounds should possess to become future drugs. In this study, we designed a series of two chemotypes of aryl-piperazine hydantoin ligands of 5-HT

Identifiants

pubmed: 39079393
pii: S0045-2068(24)00573-X
doi: 10.1016/j.bioorg.2024.107668
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

107668

Informations de copyright

Copyright © 2024 The Author(s). Published by Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Patryk Pyka (P)

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Kraków, Poland; Doctoral School of Medical and Health Sciences, Jagiellonian University Medical College, 31-530 Kraków, Poland.

Sabrina Garbo (S)

Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 324, 00161, Rome.

Aleksandra Murzyn (A)

Maj Institute of Pharmacology Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland.

Grzegorz Satała (G)

Maj Institute of Pharmacology Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland.

Artur Janusz (A)

Preclinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Michał Górka (M)

Preclinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Wojciech Pietruś (W)

Medicinal Chemistry Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Filip Mituła (F)

Preclinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Delfina Popiel (D)

Preclinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Maciej Wieczorek (M)

Preclinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland; Clinical Development Department, Celon Pharma S.A., R&D Centre, Marymoncka 15, 05-152 Kazuń Nowy, Poland.

Biagio Palmisano (B)

Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 324, 00161, Rome.

Alessia Raucci (A)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.

Andrzej J Bojarski (AJ)

Maj Institute of Pharmacology Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland.

Clemens Zwergel (C)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy; Division of Bioorganic Chemistry, School of Pharmacy, Saarland University, Campus B 2.1, D-66123 Saarbrücken, Germany.

Ewa Szymańska (E)

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

Katarzyna Kucwaj-Brysz (K)

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

Cecilia Battistelli (C)

Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 324, 00161, Rome. Electronic address: cecilia.battistelli@uniroma1.it.

Jadwiga Handzlik (J)

Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Kraków, Poland. Electronic address: j.handzlik@uj.edu.pl.

Sabina Podlewska (S)

Maj Institute of Pharmacology Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland. Electronic address: smusz@if-pan.krakow.pl.

Classifications MeSH