Development of Riluzole Analogs with Improved Use-Dependent Inhibition of Skeletal Muscle Sodium Channels.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
13 Jul 2023
Historique:
received: 21 05 2023
accepted: 20 06 2023
pmc-release: 13 07 2024
medline: 19 7 2023
pubmed: 19 7 2023
entrez: 19 7 2023
Statut: epublish

Résumé

Several commercially available and newly synthesized riluzole analogs were evaluated in vitro as voltage-gated skeletal muscle sodium-channel blockers. Data obtained from the patch-clamp technique demonstrated that potency is well correlated with lipophilicity and the introduction of a protonatable amino function in the benzothiazole 2-position enhances the use-dependent behavior. The most interesting compound, the 2-piperazine analog of riluzole (

Identifiants

pubmed: 37465302
doi: 10.1021/acsmedchemlett.3c00224
pmc: PMC10350938
doi:

Types de publication

Journal Article

Langues

eng

Pagination

999-1008

Informations de copyright

© 2023 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Alessandro Farinato (A)

Section of Pharmacology, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Maria Maddalena Cavalluzzi (MM)

Section of Medicinal Chemistry, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Concetta Altamura (C)

Section of Pharmacology, Department of Precision and Regenerative Medicine, School of Medicine, University of Bari Aldo Moro, 70124 Bari, Italy.

Carmen Campanale (C)

Section of Pharmacology, Department of Precision and Regenerative Medicine, School of Medicine, University of Bari Aldo Moro, 70124 Bari, Italy.

Paola Laghetti (P)

Section of Pharmacology, Department of Precision and Regenerative Medicine, School of Medicine, University of Bari Aldo Moro, 70124 Bari, Italy.

Ilaria Saltarella (I)

Section of Pharmacology, Department of Precision and Regenerative Medicine, School of Medicine, University of Bari Aldo Moro, 70124 Bari, Italy.

Pietro Delre (P)

CNR - Institute of Crystallography, via Amendola 122/o, 70126 Bari, Italy.

Arthur Barbault (A)

CNR - Institute of Crystallography, via Amendola 122/o, 70126 Bari, Italy.

Nancy Tarantino (N)

Section of Pharmacology, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Gualtiero Milani (G)

Section of Medicinal Chemistry, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Natalie Paola Rotondo (NP)

Section of Medicinal Chemistry, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Lorenzo Di Cesare Mannelli (L)

Department NEUROFARBA - Pharmaceutical and Nutraceutical Section, University of Firenze, 50139 Florence, Italy.

Carla Ghelardini (C)

Department NEUROFARBA - Pharmaceutical and Nutraceutical Section, University of Firenze, 50139 Florence, Italy.

Sabata Pierno (S)

Section of Pharmacology, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Giuseppe Felice Mangiatordi (GF)

CNR - Institute of Crystallography, via Amendola 122/o, 70126 Bari, Italy.

Giovanni Lentini (G)

Section of Medicinal Chemistry, Department of Pharmacy - Drug Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.

Jean-François Desaphy (JF)

Section of Pharmacology, Department of Precision and Regenerative Medicine, School of Medicine, University of Bari Aldo Moro, 70124 Bari, Italy.

Classifications MeSH