Compound (E)-2-(3,4-dihydroxystyryl)-3-hydroxy-4H-pyran-4-one downregulation of Galectin-3 ameliorates Aβ pathogenesis-induced neuroinflammation in 5 × FAD mice DOI
Xueyan Liu,

Ping Chen,

Wei Wu

et al.

Life Sciences, Journal Year: 2024, Volume and Issue: 357, P. 123085 - 123085

Published: Oct. 1, 2024

Language: Английский

Synthesis of Azirinyl Ethynyl Ketones and Their Use in the Preparation C(O)C≡CR-Substituted NH-Pyrroles/NH-Imidazoles and Azole–Azine/Azole–Azole Heterocyclic Hybrids DOI
Екатерина Е. Галенко, Vladimir A. Bodunov, Artur E. Taishev

et al.

The Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 24, 2025

Azirinyl-substituted conjugated ynones were first synthesized by the reaction of lithiated acetylenes with 2H-azirine-2-carbonyl chlorides. Azirinyl ethynyl ketones containing only a C(O)C≡CR substituent at position 2 azirine ring are good precursors for obtaining α-C(O)C≡CR substituted NH-pyrroles and 5-[C(O)C≡CR]-substituted NH-imidazoles, reacting selectively moiety 1,3-diketones arylamidines, respectively. Various N-heterocyclic hybrids (pyrrole-pyrimidine, imidazole-pyrimidine, pyrrole-isoxazole, imidazole-isoxazole, pyrimidine-pyrrole-thiophene, pyrrole-pyrimidine-thiophene, imidazole-pyrimidine-thiophene, isoxazole-pyrrole-thiophene) have been prepared based on orthogonal or domino reactions an moieties azirinyl ketones.

Language: Английский

Citations

0
Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors DOI Creative Commons
Tao Wang, Na Sun, Yuefeng Ma

et al.

ACS Pharmacology & Translational Science, Journal Year: 2025, Volume and Issue: 8(4), P. 951 - 977

Published: March 7, 2025

Cancer ranks among the top triumvirate leading causes of human deaths worldwide. The pathological mechanisms are notably intricate, demonstrating proliferative and metastatic capabilities, which complicate therapeutic interventions. sigma-1 receptor (σ1R) plays a crucial role in tumor survival migration, while sigma-2 (σ2R) is intimately associated with proliferation. This review encapsulated investigation concerning σ1R σ2R neoplasms rigorously summarized ligands radio-ligands development their applications, such as antitumor cell proliferation PET/SPECT imaging tumors. A comprehensive classification discussion was undertaken regarding chemical structures emphasized possibility dual/multitargeted ligands. Ultimately, we discussed effects chiral pharmacological characteristics on affinity pharmacokinetic features vivo, particularly radiopharmaceuticals. functions beneficial resource, fostering ligand deployment stimulating generation innovative ideas for developing

Language: Английский

Citations

0
Structure-Affinity relationships of novel σ2R/TMEM97 ligands DOI
Grant D. Walby, Qi Gu, Hongfen Yang

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 145, P. 107191 - 107191

Published: Feb. 10, 2024

Language: Английский

Citations

2
WLB-87848, a Selective σ1 Receptor Agonist, with an Unusually Positioned NH Group as Positive Ionizable Moiety and Showing Neuroprotective Activity DOI

Ute Christmann,

Lourdes Garriga,

A. Llorente

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(11), P. 9150 - 9164

Published: May 16, 2024

The synthesis and pharmacological activity of a new series thieno[2,3-

Language: Английский

Citations

2
Compound (E)-2-(3,4-dihydroxystyryl)-3-hydroxy-4H-pyran-4-one downregulation of Galectin-3 ameliorates Aβ pathogenesis-induced neuroinflammation in 5 × FAD mice DOI
Xueyan Liu,

Ping Chen,

Wei Wu

et al.

Life Sciences, Journal Year: 2024, Volume and Issue: 357, P. 123085 - 123085

Published: Oct. 1, 2024

Language: Английский

Citations

1