4773-14-2Relevant articles and documents
Dynamics and efficiency of electron injection and transport in DNA using pyrenecarboxamide as an electron donor and 5-bromouracil as an electron acceptor
Daublain, Pierre,Thazhathveetil, Arun K.,Shafirovich, Vladimir,Wang, Qiang,Trifonov, Anton,Fiebig, Torsten,Lewis, Frederick D.
, p. 14265 - 14272 (2010)
The photophysical and photochemical behavior of a series of hairpin-forming DNA conjugates possessing a 5′-tethered pyrenecarboxamide chromophore and one or two bromouracil bases has been investigated. Quenching of the pyrene fluorescence and transient absorption spectra characteristic of the pyrene cation radical are observed only when bromouracil is located at the first or second base pair position nearest to the point of pyrene attachment. These observations are consistent with an intercalated structure for these conjugates in which pyrene is adjacent to the second base pair. Selective quenching of singlet pyrene by bromouracil but not by thymine is consistent with the free energy for charge separation estimated using Weiler's equation. Low quantum yields for loss of bromide when bromouracil is not adjacent to pyrene are attributed to inefficient charge separation via either a multistep electron transport or a single-step superexchange mechanism. Quantum yields are only weakly dependent upon the distance between pyrene and bromouracil, as expected for a multistep electron transport mechanism. Loss of bromide from conjugates possessing two bromouracils occurs sequentially. For adjacent bromouracils, competitive loss of bromide from both bromouracils is observed, whereas for nonadjacent bromouracils loss of bromide from the proximal bromouracil occurs prior to any loss from the distal bromouracil, consistent with a slower rate constant for electron transport vs loss of bromide.
Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein
Mori, Mattia,Dasso Lang, Maria Chiara,Saladini, Francesco,Palombi, Nastasja,Kovalenko, Lesia,De Forni, Davide,Poddesu, Barbara,Friggeri, Laura,Giannini, Alessia,Malancona, Savina,Summa, Vincenzo,Zazzi, Maurizio,Mely, Yves,Botta, Maurizio
supporting information, p. 463 - 468 (2019/04/25)
Small molecule inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and tested in vitro 18 NC inhibitors (NCIs) bearing a double functionalization. In these NCIs, one part of the molecule is deputed to interact noncovalently with the NC hydrophobic pocket, while the second portion is designed to interact with the N-terminal domain of NC. This binding hypothesis was verified by molecular dynamics simulations, while the linkage between these two pharmacophores was found to enhance antiretroviral activity both on the wild-type virus and on HIV-1 strains with resistance to currently licensed drugs. The two most interesting compounds 6 and 13 showed no cytotoxicity, thus becoming valuable leads for further investigations.
Asymmetric aluminum complex containing acetylacetone derivative as well as preparation method and application thereof
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Paragraph 0112, (2018/05/16)
The invention discloses an asymmetric aluminum complex containing an acetylacetone derivative as well as a preparation method and application thereof. The asymmetric aluminum complex has a structuralformula shown as a formula I, wherein R1 is trifluoromethyl or methyl and R2 is phenyl, trifluoromethyl or methyl. The asymmetric aluminum complex catalyst containing the acetylacetone derivative disclosed by the invention is prepared from a ligand and trimethyl aluminum through reaction and has the advantages of simple preparation method, low cost and high product yield; the complex has a specialstructure and metal central aluminum is coordinated with divalent N, N, O and O of the ligand; the complex can be used as a catalyst for cyclic lactone ring-opening polymerization reaction and has the advantages of high catalytic activity, good stereoselectivity and rapid reaction speed; the polymerization reaction is simple to operate and an obtained polymerized product has narrow molecular weight distribution, controllable molecular weight and high yield; the asymmetric aluminum complex can be widely used for cyclic lactone ring-opening polymerization and is a very ideal catalyst. (The formula I is shown in the description.).
