4509-90-4Relevant articles and documents
Synthesis and biological activity of homologous piperidine-containing alkyl glycerolipids
Romanova,Serebrennikova,Shtil
, p. 641 - 644 (2009)
The paper provides the synthesis of new phosphorless glycerolipids with an ether bond that contain heterocyclic bases in the polar domain. The physico-chemical characteristics and biological activity of the prepared compounds were studied.
Formal synthesis of (+)-tashiromine and study toward the total synthesis of (+)-stemoamide
Chen, Yue-Jie,Bao, Rui-Yang,Zhang, Xiao-Dong,Tang, Ye-Feng
, p. 953 - 956 (2013)
An efficient formal synthesis of (+)-tashiromine was achieved by employing an intermolecular asymmetric Mannich-type reaction as the key step. Concurrently, a novel approach toward the total synthesis of (+)-stemoamide through dyotropic rearrangement of 3,4-cis-β-lactone was also explored.
Brassinosteroid-BODIPY conjugates: Design, synthesis, and properties
Malachowska-Ugarte, Magdalena,Sperduto, Claudio,Ermolovich, Yuri V.,Sauchuk, Alina L.,Jurá?ek, Michal,Litvinovskaya, Raisa P.,Straltsova, Darya,Smolich, Igor,Zhabinskii, Vladimir N.,Dra?ar, Pavel,Demidchik, Vadim,Khripach, Vladimir A.
, p. 53 - 59 (2015)
Three BS-BODIPY (brassinosteroids-4,4-difluoro-4-bora-3a,4a-diaza-s-indacene) conjugates were synthesized and their fluorescent and immunological properties were investigated. Two of the conjugates, having present all the functional groups characteristic of BS, were shown to be potentially useful as biological probes to study involvement of BS into physiological processes in living cells.
Synthesis of novel C-2- or C-15-labeled BODIPY—estrone conjugates
Bacsa, Ildikó,Konc, Csilla,Orosz, Anna Boglárka,Kecskeméti, Gábor,Rigó, Réka,zvegy-Laczka, Csilla,Mernyák, Erzsébet
, (2018)
Novel BODIPY–estrone conjugates were synthesized via Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC). Estrone-alkynes or an estrone-azide as starting compounds were synthesized via Michael addition or Sonogashira reaction as key steps. Fluorescent dyes based on BODIPY-core were provided by azide or alkyne functional groups. Fluorescent labeling of estrone was efficiently achieved at the C-2 or C-15 position. The newly-elaborated coupling procedures might have a broad applicability in the synthesis of fluorescent-labeled estrone conjugates suitable for biological assays.
PDE4 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS
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Paragraph 0331, (2021/06/22)
Provided herein are phosphodiesterase 4 (PDE4) inhibitors, e.g., a compound of Formula (I) or (II), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disease, disorder, or condition associated with PDE4 malfunction.
Targeted Delivery of mRNA with One-Component Ionizable Amphiphilic Janus Dendrimers
Zhang, Dapeng,Atochina-Vasserman, Elena N.,Maurya, Devendra S.,Liu, Matthew,Xiao, Qi,Lu, Juncheng,Lauri, George,Ona, Nathan,Reagan, Erin K.,Ni, Houping,Weissman, Drew,Percec, Virgil
supporting information, p. 17975 - 17982 (2021/11/10)
Targeted and efficient delivery of nucleic acids with viral and synthetic vectors is the key step of genetic nanomedicine. The four-component lipid nanoparticle synthetic delivery systems consisting of ionizable lipids, phospholipids, cholesterol, and a PEG-conjugated lipid, assembled by microfluidic or T-tube technology, have been extraordinarily successful for delivery of mRNA to provide Covid-19 vaccines. Recently, we reported a one-component multifunctional sequence-defined ionizable amphiphilic Janus dendrimer (IAJD) synthetic delivery system for mRNA relying on amphiphilic Janus dendrimers and glycodendrimers developed in our laboratory. Amphiphilic Janus dendrimers consist of functional hydrophilic dendrons conjugated to hydrophobic dendrons. Co-assembly of IAJDs with mRNA into dendrimersome nanoparticles (DNPs) occurs by simple injection in acetate buffer, rather than by microfluidic devices, and provides a very efficient system for delivery of mRNA to lung. Here we report the replacement of most of the hydrophilic fragment of the dendron from IAJDs, maintaining only its ionizable amine, while changing its interconnecting group to the hydrophobic dendron from amide to ester. The resulting IAJDs demonstrated that protonated ionizable amines play dual roles of hydrophilic fragment and binding ligand for mRNA, changing delivery from lung to spleen and/or liver. Replacing the interconnecting ester with the amide switched the delivery back to lung. Delivery predominantly to liver is favored by pairs of odd and even alkyl groups in the hydrophobic dendron. This simple structural change transformed the targeted delivery of mRNA mediated with IAJDs, from lung to liver and spleen, and expands the utility of DNPs from therapeutics to vaccines.
