A highly efficient [3+2] cyclization between 4-aminopyridinones and acenaphthenequinone: Access to novel acenaph-tho[1′,2':4,5]pyrrolo[3,2-c]pyridin-11-ones DOI
Xiang Zhou, Chunmei Li,

Lifeng Jiang

et al.

Tetrahedron, Journal Year: 2023, Volume and Issue: 151, P. 133815 - 133815

Published: Dec. 28, 2023

Language: Английский

Palladium-catalyzed C(sp3)-C(sp2) coupling: Synthesis of C(3)-arylphthalides DOI Creative Commons

SURYA PRAKASH RAO H,

J. Prabhakaran

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: Feb. 28, 2024

Abstract We have achieved an efficient synthesis of C(3)-arylphthalides by coupling C(3)-bromophthalides and arylboronic acids under palladium catalysis. The C(sp 3 )-C(sp 2 ) worked well in the presence water to provide products a high yield.

Language: Английский

Citations

0
The 3-(3-oxoisoindolin-1-yl)pentane-2,4-dione (ISOAC1) as a new molecule able to inhibit Amyloid β aggregation and neurotoxicity DOI Open Access
Ilaria Piccialli, Francesca Greco, Giovanni N. Roviello

et al.

Biomedicine & Pharmacotherapy, Journal Year: 2023, Volume and Issue: 168, P. 115745 - 115745

Published: Oct. 21, 2023

Amyloid β 1-42 (Aβ1-42) protein aggregation is considered one of the main triggers Alzheimer's disease (AD). In this study, we examined in vitro anti-amyloidogenic activity isoindolinone derivative 3-(3-oxoisoindolin-1-yl)pentane-2,4-dione (ISOAC1) and its neuroprotective potential against Aβ1-42 toxicity. By performing Thioflavin T fluorescence assay, Western blotting analyses, Circular Dichroism experiments, found that ISOAC1 was able to reduce conformational transition towards β-sheet structures. Interestingly, silico studies revealed bind both monomer a pentameric protofibril Aβ1-42, establishing hydrophobic interaction with PHE19 residue KLVFF motif. analyses on primary cortical neurons showed counteracted increase intracellular Ca2+ levels decreased Aβ1-42-induced toxicity, terms mitochondrial reduction reactive oxygen species production. addition, confocal microscopy intraneuronal accumulation. Collectively, our results clearly show exerts effect by reducing hence emerging as promising compound for development new Aβ-targeting therapeutic strategies AD treatment.

Language: Английский

Citations

1
Unrevealing the Nitrogen Elusive Chirality of 3‐Sulfanyl and 3‐Sulfinyl N‐Tosyl Isoindolinones by ECD Spectra: An Experimental and Theoretical Investigation DOI
Laura Palombi, Marta Monti, Erica Scarel

et al.

Chemistry - A European Journal, Journal Year: 2024, Volume and Issue: 30(29)

Published: March 18, 2024

The nitrogen-hybridization/pyramidalization of two solvated N-tosylisoindolinone derivatives having chiral residues in adjacent (I) or and distal (II) position has been investigated by a theoretical-computational procedure based on Molecular Dynamics simulations Quantum-Chemical calculations. After validation our methodology providing reliable repertory conformations modeling the electronic circular dichroism (EDC) spectra, features associated with N-pyramidalization were further characterized through Natural Bond Order (NBO) analysis. Comparing against N-geometry observed crystal structures as reference, findings reveal that presence neighbouring centers induces more pronounced solution than solid state, both I II. Furthermore, NBO analysis confirms N-lactam mostly retains sp

Language: Английский

Citations

0
Palladium-catalyzed C(sp3)-C(sp2) coupling: synthesis of C(3)-arylphthalides DOI
H. Surya Prakash Rao,

J. Prabhakaran

Chemical Papers, Journal Year: 2024, Volume and Issue: 78(10), P. 5985 - 5991

Published: May 23, 2024

Language: Английский

Citations

0
A highly efficient [3+2] cyclization between 4-aminopyridinones and acenaphthenequinone: Access to novel acenaphtho[1',2':4,5]pyrrolo[3,2-c]pyridin-11-ones DOI
Xiang Zhou, Chunmei Li,

Lifeng Jiang

et al.

Published: Jan. 1, 2023

Direct and metal-free access to poly-substituted acenaphtho[1',2':4,5]pyrrolo[3,2-c]pyridin-11-one its analogs was established through a simple one-pot reaction using enaminones acenaphthylene-1,2-dione as basic substrates. The allows the formation of C-N C-C bonds accompanied by multiple bond cleavage in presence acetic acid. approach features atomic economy, broad substrate scope, efficient conditions, inexpensive readily available starting materials easy operation, making strategy highly attractive. Importantly, new acenaphtho[1',2':4,5]pyrrolo[3,2-c]pyridin-11-ones with hydroxyl substituents could be further functionalized, affording molecular complexity diversity.

Language: Английский

Citations

0
A highly efficient [3+2] cyclization between 4-aminopyridinones and acenaphthenequinone: Access to novel acenaph-tho[1′,2':4,5]pyrrolo[3,2-c]pyridin-11-ones DOI
Xiang Zhou, Chunmei Li,

Lifeng Jiang

et al.

Tetrahedron, Journal Year: 2023, Volume and Issue: 151, P. 133815 - 133815

Published: Dec. 28, 2023

Language: Английский

Citations

0