- De-novo designed β-lysine derivatives can both augment and diminish the proliferation rates of E. coli through the action of Elongation Factor P
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An investigation into the effect of modified β-lysines on the growth rates of eubacterial cells is reported. It is shown that the effects observed are due to the post translational modification of Elongation Factor P (EFP) with these compounds catalysed b
- Connon, Stephen J.,Ghanim, Magda,Kelly, Vincent P.,McDonnell, Ciara M.,Mike Southern, J.
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- 2-AMINO-1,3,4-THIADIAZINE AND 2-AMINO-1,3,4-OXADIAZINE BASED ANTIFUNGAL AGENTS
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The invention provides a compound which is a diazine of formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt thereof, for use as an antifungal agent: (I) wherein X, N', C', A and E are as defined herein. The invention also provides a compound of Formula (I) as defined herein.
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- Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors
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The alkenyldiarylmethane (ADAM) HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are effective anti-HIV agents in cell culture. However, the potential clinical utility of the ADAMs is expected to be limited by the presence of methyl ester mo
- Silvestri, Maximilian A.,Nagarajan, Muthukaman,De Clercq, Erik,Pannecouque, Christophe,Cushman, Mark
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p. 3149 - 3162
(2007/10/03)
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- Photochemical reactions of alkoxy-containing-alkyl phenylglyoxylates: Remote hydrogen abstraction
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A series of alkoxy-containing-alkyl phenylglyoxylates have been synthesized and their photochemical reactions studied. The intention was to probe structural requirements for remote hydrogen abstraction. Products resulting from 1,10- and 1,11-hydrogen abstraction were isolated from the photochemical reactions of 4′-methoxybutyl phenylglyoxylate 3d and 5′-benzyloxypentyl phenylglyoxylate 3h respectively. Products resulting from Norrish Type II and intermolecular hydrogen abstraction reactions were also isolated. Triplet lifetimes of representative compounds were measured by laser flash photolysis.
- Hu, Shengkui,Neckers
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p. 1751 - 1754
(2007/10/03)
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- A New Oxaanalog of Myristic Acid that Suppresses Replication of Human Immunodeficiency Virus
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A series of oxaanalogs of myristic acid were synthesized and tested for antiviral activity in MT4 cells infected with human immunodeficiency virus 1 (HIV-1).The synthesized acids have no toxic effect on uninfected MT4 cells at a concentration of 100μM. 14,14,14-Trifluoro-12-oxatetradecanoic acid substantially (by 75percent) inhibits the reproduction of HIV-1.Other compounds synthesized, (7Z)-13-, (9Z)-13-, and (7Z)-11-oxatetradecenoic acids, exhibit no antiviral effect.Key words: inhibitors of retroviruses; anti-HIV agents; protein N-myristoylation; mystoylCoA: protein-N-myristoyltransferase; myristic acid; oxaanalogs; inhibitors of virus-specific protein myristoylation
- Vodovozova, E. L.,Mikhalev, I. I.,Rzhaninova, A. A.,Garaev, M. M.,Molotkovsky, Yul. G.
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p. 626 - 632
(2007/10/03)
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- Addition of Aldehydes to Activated Double Bonds, XXXIII. Syntheses and Reactions of γ-Diketones Containing Ether- or Ester Groups
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The aldehydes 1 - 8 containing ether- or ester groups are prepared by oxidation of the corresponding alcohols with pyridinium chlorochromate.Thiazolium salt-catalyzed additions of these aldehydes to vinyl ketones lead to γ-diketones 9 - 22. 2,3-O-Isopropy
- Stetter, Hermann,Leinen, Hans Theo
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p. 254 - 263
(2007/10/02)
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