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Synthesis, structure and Tuberculostatic Activity of N'-(amino-pyridyl-methylene)-hydrazinecarbodithioic Acid Methyl Esters

100%

Orlewska C.

Polish Journal of Chemistry

2001

tom Vol. 75, nr 9

1237-1245

The methods of preparation of the title esters from imidates or amidrazones are described, and structures of the compounds are elucidated on the basis of 1H, 13C-NMR, 2D-NMR spectra and X-ray diffraction method. Tuberculotic activity was also studied.

Blockade of calcium channels and AT1 receptors prevents the hypertensive effect of calcilytic NPS 2143 in rats

45%

Rybczynska A. , Jurska-Jasko A. , Boblewski K. , Lehmann A. , Orlewska C.

Journal of Physiology and Pharmacology

2010

tom 61

nr 2

Calcilytics, antagonists of calcium receptor, decrease sensitivity of this receptor to plasma calcium concentration and increase parathyroid hormone (PTH) secretion. Moreover, it was recently indicated that calcilytic NPS 2143 induces hypertension in rats. This study tested whether the increase of mean arterial blood pressure (MAP) induced by NPS 2143 administration is mediated by calcium channel and angiotensin II type1 (AT1) receptor activity. Wistar rats were anaesthesized with Thiopental i.p. and infused i.v. with saline supplemented with the anaesthetic. Blood pressure was monitored continuously in the carotid artery. Effects of NPS 2143 administered i.v. as bolus on MAP in the presence and absence of felodypine and losartan were investigated. Both, felodipine and losartan pretreatment provoked a persistent MAP decrease by 18±3 and 14±3 mmHg, respectively. Infusion of NPS 2143 at 1 mg/kg b.w. confirmed hypertensive activity of calcilytic and increased blood pressure for 21±4 mmHg. In contrast, administration of NPS 2143 in felodipine as well as in losartan pretreated rats did not change MAP as compared to felodipine/control and losartan/control groups, respectively. Our study indicated that both the blockade of calcium channels and the AT1 receptor activity prevented the hypertensive effect of calcilytic NPS 2143. This finding might be particularly important in understanding the mechanisms that mediated blood pressure changes related to the activity of calcium receptor.

Crystal and molecular structures of 1,1-bis(methylthio)-4-(2-pyridyl)-2,3,5-triaza-1,3-pentadiene and its 5-phenyl derivative

38%

Główka M. , Martynowski D. , Olczak A. , Kozłowska K. , Ołubek Z. , Orlewska C. , Foks H.

Polish Journal of Chemistry

1999

tom vol. 73 nr 5

845-851

Structures of the two dimethylthiomethylene-2-pyridinecarboxamide hydrazones have been examined spectroscopially and by X-ray diffraction to establish the dominant tautometric form and conformation. The two crystal structures are very similar with approximately planar conformation and intramolecular hydrogen bond between 4-imine group as hydrogen donor and pyridyl N atom as an acceptor. Several significant differences found may be easily explained by phenyl substitution in one of the compounds. The benzene ring in compound 2 is twisted by about 40o in relation to the mean molecular plane due to packing forces. An interesting feature of the structures is the deviation of the pyridyl ring by 11-14o from the mean 2,3,5-triaza-1,3-pentadiene plane in the two structures, despite the intramolecular hydrogen bond spanning the two fragments. It agrees with the elongation of C(4)-pyridine bond to 1.488 A, which corresponds with the lack of conjugation between p electrons of the pyridine ring and a lone pair at adjacent N(4) atom.

Formation of 4-pyridone-3-carboxamide1-β-d-ribonucleoside triphosphate in the erythrocytes, endothelium and cardiomyocytes and its effect on atp concentration

32%

Slominska E.-M. , Romaszko P. , Lipinski M. , Orlewska C. , Osman L. , Yuen A.-H. , Siedlecka U. , Foks H. , Terracciano C. , Smolenski R.-T.

Acta Biochimica Polonica

2007

tom 54

nr Supplement 4