- Palladium-catalyzed Hiyama cross-couplings of 2-chloro pyrimidines with organosilanes
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An efficient synthesis of C2-aryl pyrimidine derivatives via Pd-catalyzed Hiyama couplings has been developed. Various 2-chloro pyrimidines with electron-donating or electron-withdrawing groups as novel electrophile partners coupled well with trimethoxy(p
- Gong, Hai-Peng,Quan, Zheng-Jun,Wang, Xi-Cun
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- Interrogation of 2,2′-Bipyrimidines as Low-Potential Two-Electron Electrolytes
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As utilization of renewable energy sources continues to expand, the need for new grid energy storage technologies such as redox flow batteries (RFBs) will be vital. Ultimately, the energy density of a RFB will be dependent on the redox potentials of the respective electrolytes, their solubility, and the number of electrons stored per molecule. With prior literature reports demonstrating the propensity of nitrogen-containing heterocycles to undergo multielectron reduction at low potentials, we focused on the development of a novel electrolyte scaffold based upon a 2,2′-bipyrimidine skeleton. This scaffold is capable of storing two electrons per molecule while also exhibiting a low (~-2.0 V vs Fc/Fc+) reduction potential. A library of 24 potential bipyrimidine anolytes were synthesized and systematically evaluated to unveil structure-function relationships through computational evaluation. Through analysis of these relationships, it was unveiled that steric interactions disrupting the planarity of the system in the reduced state could be responsible for higher levels of degradation in certain anolytes. The major decomposition pathway was ultimately determined to be protonation of the dianion by solvent, which could be reversed by electrochemical or chemical oxidation. To validate the hypothesis of strain-induced decomposition, two new electrolytes with minimal steric encumbrance were synthesized, evaluated, and found to indeed exhibit higher stability than their sterically hindered counterparts.
- Griffin, Jeremy D.,Pancoast, Adam R.,Sigman, Matthew S.
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supporting information
p. 992 - 1004
(2021/01/25)
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- Structure elaboration of isoniazid: synthesis, in silico molecular docking and antimycobacterial activity of isoniazid–pyrimidine conjugates
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Abstract: Designing small molecule-based new drug candidates through structure modulation of the existing drugs has drawn considerable attention in view of inevitable emergence of resistance. A new series of isoniazid–pyrimidine conjugates were synthesize
- Kaur, Hardeep,Singh, Lovepreet,Chibale, Kelly,Singh, Kamaljit
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p. 949 - 955
(2019/11/14)
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- Primaquine-pyrimidine hybrids: Synthesis and dual-stage antiplasmodial activity
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Abstract A series of novel pyrimidine-primaquine hybrids were synthesized and their effectiveness against the blood and liver stages of malaria parasites was evaluated. The hybrids displayed enhanced liver stage in vitro activity against P. berghei liver
- Kaur, Hardeep,Machado, Marta,De Kock, Carmen,Smith, Peter,Chibale, Kelly,Prudêncio, Miguel,Singh, Kamaljit
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p. 266 - 273
(2015/07/08)
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- Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities
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The promise of hybrid antimalarial agents and the precedence set by the antimalarial drug ferroquine prompted us to design ferrocene-pyrimidine conjugates. Herein, we report the synthesis, electrochemistry and anti-plasmodial evaluation of ferrocenyl-pyrimidine conjugates against chloroquine susceptible NF54 strain of the malaria parasite Plasmodium falciparum. Also their physicochemical properties have been studied.
- Chopra, Rakesh,De Kock, Carmen,Smith, Peter,Chibale, Kelly,Singh, Kamaljit
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- Synthesis of 4-aminoquinoline - Pyrimidine hybrids as potent antimalarials and their mode of action studies
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One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of
- Singh, Kamaljit,Kaur, Hardeep,Chibale, Kelly,Balzarini, Jan
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p. 314 - 323
(2013/10/01)
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