Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na

Analgesics / chemistry Animals Binding Sites Drug Design Half-Life Humans Male Mice Mice, Transgenic Microsomes, Liver / metabolism Molecular Docking Simulation NAV1.7 Voltage-Gated Sodium Channel / chemistry Pain / chemically induced Protein Structure, Tertiary Rats Rats, Sprague-Dawley Structure-Activity Relationship Sulfonamides / chemistry Voltage-Gated Sodium Channel Blockers / chemistry

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
24 01 2019
Historique:
pubmed: 1 12 2018
medline: 18 10 2019
entrez: 1 12 2018
Statut: ppublish

Résumé

Herein, we report the discovery and optimization of a series of orally bioavailable acyl sulfonamide Na

Identifiants

DOI: 10.1021/acs.jmedchem.8b01621 PMID: 30499663
pubmed: 30499663
doi: 10.1021/acs.jmedchem.8b01621
doi:

Substances chimiques

Analgesics 0
NAV1.7 Voltage-Gated Sodium Channel 0
Sulfonamides 0
Voltage-Gated Sodium Channel Blockers 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

908-927

Auteurs

Shaoyi Sun (S)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Qi Jia (Q)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Alla Y Zenova (AY)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Michael S Wilson (MS)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Sultan Chowdhury (S)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Thilo Focken (T)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.
ORCID: 0000-0003-1993-2476

Jun Li (J)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Shannon Decker (S)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Michael E Grimwood (ME)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Jean-Christophe Andrez (JC)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Ivan Hemeon (I)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Tao Sheng (T)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Chien-An Chen (CA)

ChemPartner , Building No. 5, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , P. R. China.

Andy White (A)

ChemPartner , Building No. 5, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , P. R. China.

David H Hackos (DH)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Lunbin Deng (L)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Girish Bankar (G)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Kuldip Khakh (K)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Elaine Chang (E)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Rainbow Kwan (R)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Sophia Lin (S)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Karen Nelkenbrecher (K)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Benjamin D Sellers (BD)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.
ORCID: 0000-0002-4194-1240

Antonio G DiPasquale (AG)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Jae Chang (J)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Jodie Pang (J)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Luis Sojo (L)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Andrea Lindgren (A)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Matthew Waldbrook (M)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Zhiwei Xie (Z)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Clint Young (C)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

James P Johnson (JP)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

C Lee Robinette (CL)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Charles J Cohen (CJ)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.

Brian S Safina (BS)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.
ORCID: 0000-0001-8134-9949

Daniel P Sutherlin (DP)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Daniel F Ortwine (DF)

Genentech Inc. , 1 DNA Way , South San Francisco , California 94080-4990 , United States.

Christoph M Dehnhardt (CM)

Xenon Pharmaceuticals Inc. , 200-3650 Gilmore Way , Burnaby , British Columbia V5G 4W8 , Canada.
ORCID: 0000-0001-5213-6354

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Analgésiques › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Identification of Selective Acyl...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Identification of Selective Acyl...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Identification of Selective Acyl...
questionsmedicales.fr › Phénomènes physiques › Temps › Période › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Souris transgéniques › Identification of Selective Acyl...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Identification of Selective Acyl...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Identification of Selective Acyl...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Canaux sodiques voltage-dépendants › Canal sodique voltage-dépendant NAV1.7 › Identification of Selective Acyl...
questionsmedicales.fr › Phénomènes physiologiques de l'appareil locomoteur et du système nerveux › Phénomènes physiologiques du système nerveux › Sensation › Douleur › Identification of Selective Acyl...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Structure tertiaire des protéines › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Identification of Selective Acyl...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Identification of Selective Acyl...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Identification of Selective Acyl...
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Sulfones › Sulfonamides › Identification of Selective Acyl...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents cardiovasculaires › Bloqueurs de canaux sodiques › Bloqueurs de canaux sodiques voltage-dépendants › Identification of Selective Acyl...