Cargando…

Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro‐Oxindole Dihydroquinazolinones as IRAP Inhibitors

Insulin‐regulated aminopeptidase (IRAP) is a new potential macromolecular target for drugs aimed for treatment of cognitive disorders. Inhibition of IRAP by angiotensin IV (Ang IV) improves the memory and learning in rats. The majority of the known IRAP inhibitors are peptidic in character and suffe...

Descripción completa

Detalles Bibliográficos
Autores principales:	Engen, Karin, Vanga, Sudarsana Reddy, Lundbäck, Thomas, Agalo, Faith, Konda, Vivek, Jensen, Annika Jenmalm, Åqvist, Johan, Gutiérrez‐de‐Terán, Hugo, Hallberg, Mathias, Larhed, Mats, Rosenström, Ulrika
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	John Wiley and Sons Inc. 2020
Materias:	Full Papers
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7050655/ https://www.ncbi.nlm.nih.gov/pubmed/32154052 http://dx.doi.org/10.1002/open.201900344

Ejemplares similares

Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides
por: Borhade, Sanjay R, et al.
Publicado: (2014)

Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Aryl Sulfonamides
por: Vanga, Sudarsana Reddy, et al.
Publicado: (2018)

Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Benzopyran-Based Inhibitors
por: Vanga, Sudarsana Reddy, et al.
Publicado: (2021)

Base mediated spirocyclization of quinazoline: one-step synthesis of spiro-isoindolinone dihydroquinazolinones
por: Venkateshwarlu, Rapolu, et al.
Publicado: (2020)

Hydrogen Peroxide Induced Toxicity Is Reversed by the Macrocyclic IRAP-Inhibitor HA08 in Primary Hippocampal Cell Cultures
por: Stam, Frida, et al.
Publicado: (2022)

Ring-opening cyclization of activated spiro-aziridine oxindoles with heteroarenes: a facile synthetic approach to spiro-oxindole-fused pyrroloindolines
por: Bhandari, Sonal, et al.
Publicado: (2020)

Antitubercular, Cytotoxicity, and Computational Target Validation of Dihydroquinazolinone Derivatives
por: Venugopala, Katharigatta N., et al.
Publicado: (2022)

Synthesis of substituted 3,4-dihydroquinazolinones via a metal free Leuckart–Wallach type reaction
por: Bokale-Shivale, Suvarna, et al.
Publicado: (2020)

Studies on the Enantioselective Synthesis of E-Ethylidene-bearing Spiro[indolizidine-1,3′-oxindole] Alkaloids
por: Yayik, Nihan, et al.
Publicado: (2021)

“On-Water” Synthesis of Quinazolinones and Dihydroquinazolinones Starting from o-Bromobenzonitrile
por: Liu, Zibin, et al.
Publicado: (2018)

Spiro[pyrrolidine-3,3′-oxindoles] and Their Indoline Analogues as New 5-HT6 Receptor Chemotypes
por: Kelemen, Ádám A., et al.
Publicado: (2017)

A Facile One-Pot Construction of Succinimide-Fused Spiro[Pyrrolidine-2,3′-Oxindoles] via 1,3-Dipolar Cycloaddition Involving 3-Amino Oxindoles and Maleimides
por: Jin, Lunqiang, et al.
Publicado: (2018)

A Series of Analogues to the AT(2)R Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode
por: Isaksson, Rebecka, et al.
Publicado: (2019)

Is There an Interplay Between the Functional Domains of IRAP?
por: Vear, Anika, et al.
Publicado: (2020)

From Angiotensin IV to Small Peptidemimetics Inhibiting Insulin-Regulated Aminopeptidase
por: Hallberg, Mathias, et al.
Publicado: (2020)

Synthesis, molecular docking, and cytotoxicity of quinazolinone and dihydroquinazolinone derivatives as cytotoxic agents
por: Taayoshi, Fahimeh, et al.
Publicado: (2022)

Synthesis of spiro[dihydropyridine-oxindoles] via three-component reaction of arylamine, isatin and cyclopentane-1,3-dione
por: Sun, Yan, et al.
Publicado: (2013)

Synthesis and Bioactivity Assessment of Novel Spiro Pyrazole-Oxindole Congeners Exhibiting Potent and Selective in vitro Anticancer Effects
por: Abo-Salem, Heba M., et al.
Publicado: (2020)

Highly diastereoselective cascade [5 + 1] double Michael reaction, a route for the synthesis of spiro(thio)oxindoles
por: Moghaddam, Firouz Matloubi, et al.
Publicado: (2021)

Stereoselective Synthesis of Spiro-Decalin Oxindole Derivatives via Sequential Organocatalytic Michael–Domino Michael/Aldol Reaction
por: Straminelli, Leonardo, et al.
Publicado: (2022)

The Solubility Studies and the Complexation Mechanism Investigations of Biologically Active Spiro[cyclopropane-1,3′-oxindoles] with β-Cyclodextrins
por: Kravtsova, Anna A., et al.
Publicado: (2023)

High Contrast PET Imaging of GRPR Expression in Prostate Cancer Using Cobalt-Labeled Bombesin Antagonist RM26
por: Mitran, Bogdan, et al.
Publicado: (2017)

Gold(iii) promoted formation of dihydroquinazolinones: double X–H activation by gold
por: Kadiyala, Veerabhushanam, et al.
Publicado: (2020)

Spiro-Oxindole Skeleton Compounds Are Efficient Inhibitors for Indoleamine 2,3-Dioxygenase 1: An Attractive Target for Tumor Immunotherapy
por: Yan, Daojing, et al.
Publicado: (2022)

Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer
por: Abouzayed, Ayman, et al.
Publicado: (2019)

Graphene Oxide Catalyzed Synthesis of Fused Chromeno Spiro Pyrrolidine Oxindoles via Tandem Decarboxylation and 1,3-Dipolar Cycloaddition
por: Singh, Vipin, et al.
Publicado: (2022)

Allylation of isatin-derived N-Boc-hydrazones followed by Pd-catalyzed carboamination reaction: an entry to 3-spiro-pyrazolidyl-oxindoles
por: Gazzotti, Stefano, et al.
Publicado: (2019)

Lewis acid-catalyzed [4 + 2] cycloaddition of donor–acceptor cyclobutanes with iminooxindoles: access to spiro[piperidine-3,2′-oxindoles]
por: Chen, Zuliang, et al.
Publicado: (2022)

Chemo-/Regio-Selective Synthesis of Novel Functionalized Spiro[pyrrolidine-2,3′-oxindoles] under Microwave Irradiation and Their Anticancer Activity
por: Sharma, Richa, et al.
Publicado: (2023)

Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4
por: Ashton, Trent D., et al.
Publicado: (2023)

Heterodimeric Radiotracer Targeting PSMA and GRPR for Imaging of Prostate Cancer—Optimization of the Affinity towards PSMA by Linker Modification in Murine Model
por: Lundmark, Fanny, et al.
Publicado: (2020)

IRAP Inhibitors: M1-Aminopeptidase Family Inspiration
por: Barlow, Nicholas, et al.
Publicado: (2020)

iRAPs curb antisense transcription in E. coli
por: Magán, Andrés, et al.
Publicado: (2019)

IRAP Endosomes Control Phagosomal Maturation in Dendritic Cells
por: Weimershaus, Mirjana, et al.
Publicado: (2020)

Spiro[pyrrolidine-3, 3´-oxindole] as potent anti-breast cancer compounds: Their design, synthesis, biological evaluation and cellular target identification
por: Hati, Santanu, et al.
Publicado: (2016)

Amberlite-15 promoted an unprecedented aza Michael rearrangement for one pot synthesis of dihydroquinazolinone compounds
por: Murthy, V. Narayana, et al.
Publicado: (2018)

Evolution of Angiotensin Peptides and Peptidomimetics as Angiotensin II Receptor Type 2 (AT2) Receptor Agonists
por: Vasile, Silvana, et al.
Publicado: (2020)

Genetic diversity of Bletilla striata assessed by SCoT and IRAP markers
por: Guo, Yan, et al.
Publicado: (2018)

An Expedient Regio- and Diastereoselective Synthesis of Hybrid Frameworks with Embedded Spiro[9,10]dihydroanthracene [9,3′]-pyrrolidine and Spiro[oxindole-3,2′-pyrrolidine] Motifs via an Ionic Liquid-Mediated Multicomponent Reaction
por: Arumugam, Natarajan, et al.
Publicado: (2015)

Design of Chemically Stable, Potent, and Efficacious MDM2 Inhibitors That Exploit the Retro-Mannich Ring-Opening-Cyclization Reaction Mechanism in Spiro-oxindoles
por: Aguilar, Angelo, et al.
Publicado: (2014)

Cannot write session to /tmp/vufind_sessions/sess_ckv6v3b3fk7kaqg30fe2il387s