A convergent route toward nitrogen-bridged BODIPY oligomers has been developed. The synthetic key step is a Buchwald-Hartwig cross-coupling reaction of an α-amino-BODIPY and the respective halide. Not only does the selective synthesis provide control of the oligomer size, but the facile preparative procedure also enables easy access to these types of dyes. Furthermore, functionalized examples were accessible via brominated derivatives.
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http://dx.doi.org/10.1021/acs.orglett.4c00827 | DOI Listing |
Org Lett
April 2024
DFG Cluster of Excellence livMatS @FIT and Albert-Ludwigs-Universität Freiburg, Institute of Organic Chemistry, Albertstraße 21, 79104 Freiburg im Breisgau, Germany.
A convergent route toward nitrogen-bridged BODIPY oligomers has been developed. The synthetic key step is a Buchwald-Hartwig cross-coupling reaction of an α-amino-BODIPY and the respective halide. Not only does the selective synthesis provide control of the oligomer size, but the facile preparative procedure also enables easy access to these types of dyes.
View Article and Find Full Text PDFMikrochim Acta
November 2023
School of Chemistry, Xi'an Jiaotong University, Xi'an, 710049, China.
A sensitive and accurate chemiluminescence (CL) method was developed for one-step determination of diphenyl ether herbicides at trace level with nitrofen (2,4-dichlorophenyl-p-nitrophenyl ether) as a model analyte. Candida rugosa lipase (CRL) was immobilized on a nanocarrier of amine-linked covalent organic framework (named as COF-300-AR) through a self-assembly strategy. The formed nanocomposite of COF-300-AR@CRL owns dual enzymatic catalytic activities.
View Article and Find Full Text PDFJ Med Chem
November 2020
National Engineering Research Center for the Emergency Drug, State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
A series of novel linear aliphatic amine-linked triaryl derivatives as inhibitors of PD-1/PD-L1 were designed, synthesized, and evaluated in vitro and in vivo. In this chemical series, compound showed the most potent inhibitory activity and binding affinity with hPD-L1, with an IC value of 12 nM and a KD value of 16.2 pM, showing a binding potency approximately 2000-fold that of hPD-1.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
August 2019
National Science Foundation (NSF)-National Aeronautics and Space Administration (NASA) Center for Chemical Evolution, Atlanta, GA 30332;
Numerous long-standing questions in origins-of-life research center on the history of biopolymers. For example, how and why did nature select the polypeptide backbone and proteinaceous side chains? Depsipeptides, containing both ester and amide linkages, have been proposed as ancestors of polypeptides. In this paper, we investigate cationic depsipeptides that form under mild dry-down reactions.
View Article and Find Full Text PDFEur J Med Chem
December 2012
Dipartimento di Farmacia, Università degli Studi di Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.
Alzheimer's disease (AD) onset and progression are associated with the dysregulation of multiple and complex physiological processes and a successful therapeutic approach should therefore address more than one target. Two new chemical entities, the easily accessible heterocyclic scaffolds 1,3-diphenylbenzo[e][1,2,4]triazin-7(1H)-one (benzotriazinone I) and 2-phenyl-6H-[1,2,4]triazino[5,6,1-jk]carbazol-6-one (triazafluoranthenone II), were explored for their multitarget-directed inhibition of beta-amyloid (Aβ) fibrillization and acetyl- (AChE) and/or butyryl- (BChE) cholinesterase, three valuable targets for AD therapy. Introduction of appropriate amine substituents at positions 6 and 5 on scaffold I and II, respectively, allowed the preparation of a series of compounds that were tested as Aβ(1-40) aggregation and cholinesterase inhibitors.
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