Novel heterocycle-fused thyromimetics are presented carrying indoles or indazoles instead of the phenolic group in T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. Moderate THRbeta selectivity (approx. 10-fold) was observed in the indole series using isoform-selective transient THR transfection assays.
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http://dx.doi.org/10.1016/j.bmcl.2005.02.028 | DOI Listing |
Inorg Chem
January 2025
Key Laboratory of Polyoxometalate Science of Ministry of Education, Faculty of Chemistry, Northeast Normal University, Changchun, Jilin 130024, PR China.
Two novel 3D inorganic-organic hybrids based on [VO]/[VO] clusters, [Cu(bbpy)(VO)]·3HO () and [CuAg(pty)(VO)]·HO () (bbpy = 3,5-bis(1-benzimidazole) pyridine, pty = 4'-(4″-pyridyl)-2,2':6',2″-terpyridine), were isolated in the same POV/Cu/N-heterocycle ligand reaction systems. Hybrids and possess novel three-dimensional bimetallic frameworks derived from [VO]/[VO] clusters and Cu-organic complexes. In , bbpy ligands are grafted by Cu to a grid ribbon 2D sheet, which are connected with benzene-like [VO] to yield a 3D framework.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
University of Toronto, Dept. of Chemistry, 80 St. George Street, M5S 3H6, Toronto, CANADA.
A copper-catalyzed enantioselective synthesis of borylated 1-pyrrolines from γ,δ-unsaturated oxime esters is reported. Twenty-four novel 1-pyrroline derivatives are reported in yields ranging from 26% to 96% and enantioselectivities from 74.5:25.
View Article and Find Full Text PDFMol Biochem Parasitol
January 2025
Post-graduate Program in Pharmaceutical Sciences, Federal University of Ceará, Fortaleza - CE, Brazil; Fundação Oswaldo Cruz, Fiocruz, Fiocruz Ceará, Eusébio - CE, Brazil; Northeast Network of Biotechnology (RENORBIO), State University of Ceará (UECE), Fortaleza - CE, Brazil.
Globally, an estimated 1 billion people reside in endemic areas, and over 12 million individuals are infected with leishmaniasis. Despite its prevalence, leishmaniasis continues to be a neglected disease, mainly affecting underdeveloped countries. In Brazil, the available treatments are pentavalent antimonials and Amphotericin B, which are outdated, toxic, require prolonged parenteral administration and have limited efficacy.
View Article and Find Full Text PDFArch Pharm (Weinheim)
January 2025
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, Italy.
In the last few years, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been the cause of a worldwide pandemic, highlighting the need for novel antiviral agents. The main protease (M) of SARS-CoV-2 was immediately identified as a crucial enzyme for viral replication and has been validated as a drug target. Here, we present the design and synthesis of peptidomimetic M covalent inhibitors characterized by quinoline-based P moieties.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
University of Bari: Universita degli Studi di Bari Aldo Moro, Dept. of Pharmacy - Drug Sciences, via E. Orabona 4, 70125, Bari, ITALY.
Strained spiro-heterocycles (SSH) have gained significant attention within the medicinal chemistry community as promising (sp3)-rich bioisosteres for their aromatic and non-spirocyclic counterparts. We herein report access to an unprecedented spiro-heterocycle - 1,5-dioxaspiro[2.3]hexane.
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