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Understanding the Ligand Influence in the Multistep Reaction of Diazoalkanes with Palladium Complexes Leading to Carbene-Aryl Coupling.

Organometallics

January 2025

IU CINQUIMA/Química Inorgánica, Universidad de Valladolid, Valladolid 47071, Spain.

The reaction of diphosphino aryl complexes [Pd(CF)(L-L)(NCMe)](BF) (L-L = dppe, dppp, dppb) with diazoalkanes NCHR ( = -CH=CHPh, Ph) leads to η-allyl or η-benzyl palladium derivatives that are the organometallic products resulting from carbene-aryl coupling. The experimental trend shows that the reaction is favored for dppe > dppp > dppb. It involves several consecutive steps, i.

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Previous studies showed that the female genital tract microbiome plays a crucial role in regulating the host's immune defense mechanisms. Our previous research has shown that Lactobacillus gasseri LGV03 (L. gasseri LGV03) isolated from cervico-vagina of HPV-cleared women contributes to clearance of HPV infection and beneficially regulate immune response.

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Discovery of pyrazoline analogs as multi-targeting cholinesterase, β-secretase and Aβ aggregation inhibitors through lead optimization strategy.

Int J Biol Macromol

January 2025

Pharmaceutical Chemistry Research Laboratory I, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India. Electronic address:

The multi-target directed ligands (MTDLs) strategy has been evolved as the propitious approach for the development of therapeutics for Alzheimer's disease (AD). In an earlier report, we described the novel series of chalcone derivatives bearing N-aryl piperazine scaffold as MTDLs for the treatment of AD. Herein, we report the lead optimization of the series culminating in potent, multi-targeting compounds (32-57), evaluated through in-vitro and in-vivo biological studies.

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High-Throughput Zebrafish Screening Reveals Cardiotoxic Effects of Organophosphate Flame Retardants.

Environ Res

January 2025

International Research Center for Marine Biosciences, Shanghai Ocean University, Ministry of Science and Technology, Shanghai 201306, P.R. China; Key Laboratory of Exploration and Utilization of Aquatic Genetic Resources, Ministry of Science and Technology, Shanghai Ocean University, Shanghai 201306, P.R. China; Marine Biomedical Science and Technology Innovation Platform of Lin-gang Special Area, Shanghai 201306, P.R. China. Electronic address:

The toxicity of organophosphorus flame retardants (OPFRs) remains poorly understood, despite their widespread environmental presence and potential risks to human and ecological health. This study aimed to characterize the cardiovascular developmental toxicity of OPFRs using a high-throughput zebrafish screening model. Over thirty representative OPFRs, classified into three major groups-alkyl, aryl, and halogenated-were evaluated.

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Modular Access to Chiral Benzylamines via Ni/Photoredox-Catalyzed Multicomponent Cross-Electrophile Coupling.

Org Lett

January 2025

School of Chemistry and Chemical Engineering, Nanchang University, Nanchang, Jiangxi 330031, P. R. China.

A Ni/photoredox dual-catalyzed multicomponent cross-electrophile coupling of N-vinyl amides with (hetero)aryl halides and (2°, 3°)-alkyl redox-active esters in the presence of cheap reductant Hantzsch ester is reported here. This reductive protocol provides direct access to various synthetically challenging chiral α-arylamides in good yields and excellent enantioselectivities (up to 99% ee, with the majority exceeding 97% ee), which can be further derived into chiral primary and secondary amines. Preliminary experimental studies shed light on the potential catalytic pathways.

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