N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.

Animals Disease Models, Animal Dose-Response Relationship, Drug Hepatocytes / chemistry Ligands Male Mice Mice, Inbred Strains Microsomes, Liver / chemistry Models, Molecular Molecular Structure Receptor, Angiotensin, Type 2 / agonists Spinal Cord / drug effects Structure-Activity Relationship Sulfonamides / chemical synthesis Thiophenes / chemical synthesis Vasodilation / drug effects
AT(2)R ligands Angiotensin II type 2 receptor Carboxylic acid bioisosteres Liver microsomes Sulfonyl carbamates

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 01 2021
Historique:
received: 16 09 2020
revised: 29 10 2020
accepted: 31 10 2020
pubmed: 15 12 2020
medline: 31 7 2021
entrez: 14 12 2020
Statut: ppublish

Résumé

A series of meta-substituted acetophenone derivatives, encompassing N-(alkyloxycarbonyl)thiophene sulfonamide fragments have been synthesized. Several selective AT2 receptor ligands were identified, among those a tert-butylimidazole derivative (20) with a K

Identifiants

DOI: 10.1016/j.bmc.2020.115859 PMID: 33309749
pubmed: 33309749
pii: S0968-0896(20)30689-1
doi: 10.1016/j.bmc.2020.115859
pii:
doi:

Substances chimiques

Ligands 0
Receptor, Angiotensin, Type 2 0
Sulfonamides 0
Thiophenes 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

115859

Informations de copyright

Copyright © 2020 Elsevier Ltd. All rights reserved.

Auteurs

Johan Wannberg (J)

Department of Medicinal Chemistry, Science for Life Laboratory, BMC, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.

Johan Gising (J)

The Beijer Laboratory, Department of Medicinal Chemistry, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden.

Jens Lindman (J)

The Beijer Laboratory, Department of Medicinal Chemistry, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden.

Jessica Salander (J)

Department of Cell and Molecular Biology, BMC, Box 596, Uppsala University, SE-751 24 Uppsala, Sweden.

Hugo Gutiérrez-de-Terán (H)

Department of Cell and Molecular Biology, BMC, Box 596, Uppsala University, SE-751 24 Uppsala, Sweden.

Hanin Ablahad (H)

The Beijer Laboratory, Department of Pharmaceutical Biosciences, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden; Department of Pharmacology and Biomedicine Discovery Institute, Monash University, Clayton 3800, VIC, Australia.

Selin Hamid (S)

The Beijer Laboratory, Department of Pharmaceutical Biosciences, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden; Department of Pharmacology and Biomedicine Discovery Institute, Monash University, Clayton 3800, VIC, Australia.

Alfhild Grönbladh (A)

The Beijer Laboratory, Department of Pharmaceutical Biosciences, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden.

Iresha Spizzo (I)

Department of Pharmacology and Biomedicine Discovery Institute, Monash University, Clayton 3800, VIC, Australia.

Tracey A Gaspari (TA)

Department of Pharmacology and Biomedicine Discovery Institute, Monash University, Clayton 3800, VIC, Australia.

Robert E Widdop (RE)

Department of Pharmacology and Biomedicine Discovery Institute, Monash University, Clayton 3800, VIC, Australia.

Anders Hallberg (A)

Department of Medicinal Chemistry, Uppsala University, BMC, Box 574, 751 23 Uppsala, Sweden.

Maria Backlund (M)

Department of Pharmacy, Uppsala University, Uppsala, Sweden; Uppsala University Drug Optimization and Pharmaceutical Profiling Platform (UDOPP), Science for Life Laboratory, Uppsala, Sweden.

Anna Leśniak (A)

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

Mathias Hallberg (M)

The Beijer Laboratory, Department of Pharmaceutical Biosciences, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden.

Mats Larhed (M)

Department of Medicinal Chemistry, Science for Life Laboratory, BMC, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden; The Beijer Laboratory, Department of Medicinal Chemistry, Uppsala University, BMC, Box 591, 751 24 Uppsala, Sweden. Electronic address: mats.larhed@ilk.uu.se.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles biologiques › Modèles animaux de maladie humaine › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Cellules › Cellules épithéliales › Hépatocytes › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteurs aux angiotensines › Récepteur de type 2 à l'angiotensine-II › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Système nerveux › Système nerveux central › Moelle spinale › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Sulfones › Sulfonamides › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Thiophènes › N-(Methyloxycarbonyl)thiophene sulfonamides as...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiologiques cardiovasculaires › Hémodynamique › Vasodilatation › N-(Methyloxycarbonyl)thiophene sulfonamides as...