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Günther Entenmann Emil Eckle John J. Stezowski 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3):303-308
Abstract Several 2-hydroximino-1,3-thiazolidine-4-ones have been prepared by reaction of the respective α-thiocyanatocarbonic acid esters with hydroxylamine. They have been characterized by ir, uv and 1H-nmr. The chemical structure was determined unequivocally by the crystal structure analysis of 5-ethyl-2-hydroximino-1,3-thiazolidine-4-one, space-group: P21/c, a = 10.0382(7), b = 5.2903(4), c = 19.305(1) Å, β = 134.233(4) at T = 24(1)°C. The structural model was refined with 3196 data to give R = 0.044. Analysis of the bonding geometry has lead to characterization of the 2-amino-1,3-thiazolidine-4-ones as cyclic N-thiaiminoamides. 相似文献
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Opletalova V Dolezel J Kralova K Pesko M Kunes J Jampilek J 《Molecules (Basel, Switzerland)》2011,16(6):5207-5227
A series of rhodanine derivatives was prepared. The synthetic approach, analytical and spectroscopic data of all synthesized compounds are presented. Lipophilicity of all the discussed rhodanine derivatives was analyzed using the RP-HPLC method. The compounds were tested for their ability to inhibit photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts and reduce chlorophyll content in freshwater alga Chlorella vulgaris. Structure-activity relationships between the chemical structure, physical properties and biological activities of the evaluated compounds are discussed. For majority of the tested compounds the lipophilicity of the compound and not electronic properties of the R1 substituent were decisive for PET-inhibiting activity. The most potent PET inhibitor was (5Z)-5-(4-bromobenzylidene)-2-thioxo-1,3-thiazolidin-4-one (IC(50) = 3.0 μmol/L) and the highest antialgal activity was exhibited by (5Z)-5-(4-chlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one (IC(50) = 1.3 μmol/L). 相似文献
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N. M. Turkevich E. V. Vladzimirskaya L. M. Vengrinovich 《Chemistry of Heterocyclic Compounds》1969,5(3):376-378
The C=O groups in positions 4 of the molecules of 2-thioxo-1, 3-thiazan-4-one and 1,3-thiazane-2,4-dione do not possess ketonic properties. When 2-thioxo-1,3-thiazan-4-one is treated with hydrazine or its derivatives, hydrazinolysis takes place. When these substances react with P2S5, the C=O groups are replaced by C=S groups. The compounds formed possess thioketonic properties, which makes it possible to obtain derivatives of 4-imino-1,3-thiazane. The condensation of -chloropropionic acid with thiourea leads to 1,3-thiazane-2,4-dione and the previously unreported 2-imino-1,3-thiazan-4-one. The UV spectra of the substances synthesized are described. 相似文献
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Lee LV Bower KE Liang FS Shi J Wu D Sucheck SJ Vogt PK Wong CH 《Journal of the American Chemical Society》2004,126(15):4774-4775
The anthrax lethal factor (LF), a Zn-dependent endopeptidase, is considered the dominant virulence factor of anthrax. Because pharmacological inhibition of the catalytic activity of LF is considered a plausible mechanism for preventing the lethality of anthrax, a high-throughput screening experiment based on LF-catalyzed cleavage of a fluorescent substrate was performed to identify novel inhibitors of LF. The RNA-targeting antibiotics, neomycin B and some synthetic dimeric aminoglycosides, were found to be nanomolar active-site inhibitors of LF. 相似文献
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A series of novel cyclic urea molecules 5,6-dihydroxy-1,3-diazepane-2,4,7-trione as HIV-1 protease inhibitors were designed
using computational techniques. The designed molecules were compared with the known cyclic urea molecules by performing docking
studies, calculating their ADME (Absorption, Distribution, Metabolism, and Excretion) properties and protein ligand interaction
energy. These novel molecules were designed by substituting the P
1/P′
1 positions (4
th
and 7
th
position of 1, 3-diazepan-2-one) with double bonded oxygens. This reduces the molecular weight and increases the bioavailability,
indicating better ADME properties. The docking studies showed good binding affinity towards HIV-1 protease. The biological
activity of these inhibitors were predicted by a model equation generated by the regression analysis between biological activity
(log 1/K
i
) of known inhibitors and their protein ligand interaction energy. The synthetic studies are in progress.
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