Chemical and biological properties of some derivatives of cis-and trans-1-hydroxyquinolizidine

1968 ◽  
Vol 11 (2) ◽  
pp. 353-357 ◽  
Author(s):  
James D. England ◽  
Davis Temple ◽  
Joseph Sam
2017 ◽  
Vol 18 (5) ◽  
pp. 1739-1746
Author(s):  
D. L. Gallagher ◽  
K. Phetxumphou ◽  
A. M. Dietrich

Abstract Chemical spills polluting drinking water are often mixtures with each chemical having unique characteristics for partitioning, toxicity, and odour leading to significant differences in human risk exposures. A 2014 chemical spill of crude (4-methylcyclohexyl)methanol (MCHM) resulted in a $126 million USD fine to the water utility. The spill consisted of at least ten chemicals including 34% cis- and 60% trans-4-MCHM and 0.7% cis- and 0.3% trans-methyl-4-methylcyclohexanecarboxylate (MMCHC). While a very minor component, trans-MMCHC contributed substantially to odour because of its high Henry's Law Constant, 2.23 × 10−2 at 40 °C showering, and low odour threshold concentration (OTC), 0.02 ppb-v, air. Using USEPA risk assessment parameters in a 15-minute shower model with influent concentration of 42 ppb-aq cis- and trans-4-MMCHC, representative of initial spill concentrations in the distribution system, adult ingestion and inhalation for trans-MMCHC were almost equal, 4.00 × 10−4 and 4.26 × 10−4 mg/kg/d, respectively. For children, inhalation doses exceeded ingestion dose: 1.72 × 10−3 mg/kg/d versus 0.93 × 10−3 mg/kg/day trans-MMCHC. This exposure assessment with varying OTC for crude MCHM chemicals reinforces considering chemical, physical, and biological properties of all chemicals in the spill. Consumers aware of their exposure to chemicals in drinking water lost consumer confidence; the water utility was required to compensate individuals and businesses for financial losses.


2005 ◽  
Vol 31 (5) ◽  
pp. 482-494 ◽  
Author(s):  
A. I. Nazarova ◽  
A. V. Feofanov ◽  
T. A. Karmakova ◽  
G. V. Sharonov ◽  
A. D. Plyutinskaya ◽  
...  

2021 ◽  
Vol 55 (2 (255)) ◽  
pp. 103-111
Author(s):  
Tariel V. Ghochikyan ◽  
Armen S. Galstyan ◽  
Hrachik M. Stepanyan ◽  
Irina G. Korpakova ◽  
Alexander S. Kinzirsky

Based on carbonyl derivatives of 4-substituted-4-butanolides, the appropriate semi- and thiosemicarbazones have been synthesized. It has been found that some representatives of thiosemicarbazones have pronounced algicidal activity against filamentous green alga Cladophora and blue-green alga (cyanobacterium) Synechocystis and some of the semi- and thiosemicarbazones exhibit moderate antitumor activity. The assessment of the antitumor activity of the compounds was carried out using strains of syngeneic and allogeneic tumor systems as test-objects: lymphocytic leukemia P-388, Lewis lung carcinoma, B16 melanoma and Ehrlich’s ascites tumor. It has also been established that some representatives of thiosemi­carbazones exhibit antimutagenic properties. It has been reliably proven that with the formation of a thiazole ring, all properties disappear and a new property in the series of thiazololactones is revealed – antibacterial․


2021 ◽  
Vol 18 ◽  
Author(s):  
Sarah Kappler ◽  
Andreas Siebert ◽  
Uli Kazmaier

Introduction: Miuraenamides belong to marine natural compounds with interesting biological properties. Materials and Methods: They initiate polymerization of monomeric actin and therefore show high cytotoxicity by influencing the cytoskeleton. New derivatives of the miuraenamides have been synthesized containing a N-methylated amide bond instead of the more easily hydrolysable ester in the natural products. Results: Incorporation of an aromatic side chain onto the C-terminal amino acid of the tripeptide fragment also led to highly active new miuraenamides. Conclusion: We could show that the ester bond of the natural product miuraenamide can be replaced by an N-methyl amide. The yields in the cyclization step are high and generally much better that with the corresponding esters. On the other hand, the biological activity of the new amide analogs are lower compared to the natural products, but the activity can significantly be increased by incorporation of a p-nitrophenyl group at the C-terminus of the peptide fragment.


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