| 1. |
- Batta, Gy., et al.
(författare)
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C‐19 configurational assignments in some morphine derivatives by homonuclear NOE
- 1992
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Ingår i: Magnetic Resonance in Chemistry. - : Wiley. - 0749-1581 .- 1097-458X. ; 30:13, s. S96-S104
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Tidskriftsartikel (refereegranskat)abstract
- Azidolysis‐thermolysis of C‐19 diastereomer tosyl esters of morphine derivatives resulted in the formation of a new substituted 4‐azatetracyclo [4.4.02,4.03,8] decane ring system. As the course of such transformations depends on the chirality of C‐19, its relative configuration was determined both in the starting materials and in the new compounds. To this end a semiquantitative 1H{1H} NOE interpretation was combined with MMX molecular mechanics. Interestingly, both in the starting materials with a rotating C‐7—C‐19 bond and in the fairly rigid aziridine ring‐containing products, the same (H‐8α{19‐Me}) NOE effects were the most informative on the stereochemistry. In addition full a priori 1H and 13C assignments of 13 compounds are presented.
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| 2. |
- Chang-Chun, Chen, et al.
(författare)
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Nucleoside transport inhibition mediates lidoflazine-induced cardioprotection during intermittent aortic crossclamping
- 1992
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Ingår i: Journal of Thoracic and Cardiovascular Surgery. - : Elsevier. - 0022-5223 .- 1097-685X. ; 104:6, s. 1602-1609
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Tidskriftsartikel (refereegranskat)abstract
- The effects of pretreatment with the nucleoside transport inhibitor lidoflazine on repeated ischemia-reperfusion injury induced by normothermic intermittent aortic crossclamping were studied in canine hearts. Eighteen mongrel dogs were allocated to three groups: placebo (n = 6), lidoflazine (1 mg/kg) (n = 6), and lidoflazine (1 mg/kg) plus the adenosine receptor blocker aminophylline (7 mg/kg) (n = 6). Pretreatment was performed intravenously during 15 minutes before extracorporeal circulation. All hearts were subjected to four intervals of 15 minutes of global ischemia each followed by 10 minutes of reperfusion. After weaning from extracorporeal circulation, functional recovery was followed for 1 hour. In the lidoflazine group, myocardial adenosine content (0.25 +/- 0.06 mumol/gm dry weight) was 3.5 times higher than that in the control group (0.07 +/- 0.03 mumol/gm dry weight; p < 0.05) at the end of the last aortic crossclamping. The release of adenosine from the myocardium during each reperfusion period was significantly higher than that in the control group (p < 0.05). Myocardial extraction of lactate was normalized at every reperfusion interval in the lidoflazine group but not in the control group (p < 0.05). In the lidoflazine group functional recovery was significantly better than that in the control group. Positive rate of rise of pressure, negative rate of rise of pressure, and cardiac output recovered to, respectively, 150% +/- 19%, 82% +/- 8%, and 131% +/- 15% in the lidoflazine group versus, respectively, 37% +/- 9%, 23% +/- 7%, and 29% +/- 8% in the control group (p < 0.001) at 1 hour after extracorporeal circulation. When the adenosine receptor blocker aminophylline was administered in association with lidoflazine, protection dropped significantly: positive and negative rate of rise of pressure and cardiac output were, respectively, 58% +/- 8%, 46% +/- 9%, and 67% +/- 16% at 1 hour after extracorporeal circulation (p < 0.05 versus lidoflazine alone). These results suggest that the cardioprotective effects of lidoflazine are at least in part mediated by adenosine receptor stimulation via nucleoside transport inhibition-induced accumulation of endogenous adenosine in the myocardium.
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| 3. |
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| 4. |
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| 5. |
- Csende, F., et al.
(författare)
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Synthesis and structural study of new saturated isoindol-1-one derivatives
- 1993
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Ingår i: Heterocycles. - : The Japan Institute of Heterocyclic Chemistry. - 0385-5414 .- 1881-0942. ; 36:8, s. 1809-1821
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Tidskriftsartikel (refereegranskat)abstract
- Condensation of 2-p-toluoylcyclohexanecarboxylic acid (1a,b) with primary amines gave the corresponding hexahydroisoindol-1-ones (2a-g) in good yield. The octahydro derivatives (4a-g) were prepared from cis- and trans-hexahydro-1(2H)-phthalazinone (3a,b) by reduction with zinc-hydrochloric acid via ring contraction. Stereoselective synthesis of cis-N-phenyloctahydroisoindol-1-one (4h) was performed starting from 2b by reduction with magnesium-methanol at room temperature. Configurational assignments of cis and trans isomers were based on 1H-and 13C-nmr spectroscopic studies.
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| 6. |
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| 7. |
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| 8. |
- Kóródi, F., et al.
(författare)
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Fused 1,2,4-triazole heterocycles. I. Synthesis of novel [1,2,4]triazolo[5′,1′:2,3][1,3]thiazino[6,5-b]quinolines
- 1992
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Ingår i: Heterocycles. - : The Japan Institute of Heterocyclic Chemistry. - 0385-5414 .- 1881-0942. ; 34:9, s. 1711-1720
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Tidskriftsartikel (refereegranskat)abstract
- Derivatives of a new heterocyclic ring system of [1,2,4]triazolo[5′,1′: 2,3][1,3]thiazino[6,5-b]quinolines (4,5,6,7 and 8) have been synthesised by the reaction of 2-chloroquinoline-3-carbaldehyde derivatives (1 and 2) with 1,2,4-triazole-5-thiols (3), and subsequent transformations of the hydroxy group of 11-hydroxy[1,2,4]triazolo[5′,1′: 2,3][1,3]thiazino[6,5-b]quinoline (4a).
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| 9. |
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| 10. |
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| 11. |
- Marton, J., et al.
(författare)
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Herstellung von 6,14‐Ethenomorphinan‐Derivaten
- 1993
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Ingår i: Liebigs Annalen der Chemie. - : Wiley. - 0170-2041 .- 1099-0690. ; 1993:8, s. 915-919
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Tidskriftsartikel (refereegranskat)abstract
- Preparation of 6,14‐Ethenomorphinane Derivatives Buprenorphine (5j) and diprenorphine (5k) were synthesized from N‐formyl‐northebaine (1c) and N‐benzyl‐northebaine (1d) via new intermediates. N‐cyclopropylmethyl‐dihydronorthevinone 3d is a suitable compound for the synthesis of both 5j and 5k. We carried out detailed 1H‐ and 13C‐NMR analysis of the new compounds.
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| 12. |
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| 13. |
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| 14. |
- Szabo, Zoltan, Associate professor, et al.
(författare)
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1H and 13C NMR study of novel fused 1,2,4‐triazole heterocycles
- 1992
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Ingår i: Magnetic Resonance in Chemistry. - : Wiley. - 0749-1581 .- 1097-458X. ; 30:11, s. 1111-1116
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Tidskriftsartikel (refereegranskat)abstract
- The 1H and 13C NMR spectra of some novel 1,2,4‐triazolo [1,3] thiazinoquinoline isomeric pairs are interpreted in terms of structural assignments. The structure of most compounds has been confirmed by NOE difference spectroscopy. Characteristic differences have been observed in both 1H and 13C NMR spectra of these isomeric Pairs: some of the 1H and 13C chemical shifts, and also the one bond 13C1H couplings of triazole protons, differ consistently in the NMR spectra of the isomers. The coupling constants have been determined using a combination of INEPT and chemical shift selective filtering.
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| 15. |
- Szabó, Zoltan, Associate professor, et al.
(författare)
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Interpretation of the 13C NMR spectra of 3‐benzylideneflavanones, 3‐benzylflavone and 3‐benzyl‐1‐thioflavone derivatives
- 1993
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Ingår i: Magnetic Resonance in Chemistry. - : Wiley. - 0749-1581 .- 1097-458X. ; 31:4, s. 418-421
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Tidskriftsartikel (refereegranskat)abstract
- 13C NMR spectra of 3‐benzylflavones, 3‐benzylideneflavanones, 3‐benzyl‐4‐thioflavones, 3‐benzyl‐1‐thioflavones, 3‐benzyl‐1,4‐dithioflavones and 3‐benzyl‐1‐thioflavone‐1,1‐dioxides were analysed and correlated to evaluate the consequences of the replacement of oxygen with sulphur.
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| 16. |
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| 17. |
- Szabó, Zoltan, Associate professor, et al.
(författare)
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Synthesis and biological activity of 4‐aikoxy‐ and 4‐ω‐aminoalkoxy‐2‐trichloromethylquinolines
- 1991
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Ingår i: Pesticide science. - : Wiley. - 0031-613X .- 1096-9063. ; 31:3, s. 263-271
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Tidskriftsartikel (refereegranskat)abstract
- A number of new 4‐alkoxy‐ and 4‐ω‐aminoalkoxy‐2‐trichloromethyl‐quinolines were synthesised and tested on insects, weeds and plant pathogens. Many of these compounds showed antifungal activity against different fungal species. Some compounds, IVa, IVb, IVc, Vb, Vc and VI, had interesting effects on Phycomycete fungi.
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| 18. |
- Szecsi, J, et al.
(författare)
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[Effect of acute aprotinin (Gordox) therapy on hemostasis in heart surgery patients, with special reference to hyperfibrinolysis] : [Article in Hungarian]
- 1990
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Ingår i: Orvosi Hetilap. - : Akademiai Kiado Rt.. - 0030-6002 .- 1788-6120. ; 131:51, s. 2809-2814
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Tidskriftsartikel (refereegranskat)abstract
- Authors have studied the effect of Gordox-therapy on haemostasis after open heart surgery in a prospective clinical trial. Thirty seven patients (pts) undergoing cardiac surgery due to their valve disease were randomly assigned either to control-group (20 pts) or to Gordox-group (17 pts). The patients in the Gordox group were given Gordox according the following scheme: 2 M IU within 20 min. after induction of anaesthesia followed by 0.5 M IU/hour infusion until the end of the operation. One M IU also was given into the oxygenator before starting the extracorporeal circulation. The postoperative chest tube drainage was less in Gordox-group (534 +/- 260 ml vs. 987 +/- 583 ml, p less than 0.005), and donor blood and fresh frozen plasma requirement was also lower in this group (534 +/- 633 ml vs. 935 +/- 718 ml p less than 0.05; 70 +/- 153 ml vs. 211 +/- 245 ml p less than 0.05, respectively). There was no significant difference between the two groups concerning the postoperative activated partial thromboplastin time, prothrombin time, thrombin time values. The authors could document significantly higher fibrinogen concentration and significantly lower fibrinolytic activity postoperatively in the Gordox-group (p less than 0.05). Gordox therapy has advantageous effect on haemostasis after open heart surgery which can be documented both by clinical and laboratory examination.
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| 19. |
- Tóth, I., et al.
(författare)
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Extraction of gallium(III) and aluminium(III) with O,O-dialkyldithiophosphoric acids
- 1990
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Ingår i: Talanta. - : Elsevier BV. - 0039-9140 .- 1873-3573. ; 37:12, s. 1175-1178
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Tidskriftsartikel (refereegranskat)abstract
- The extraction of Ga3+ and Al3+ with the liquid cation-exchangers di-n-butyldithiophosphoric acid (DBTPA) and di-(2-ethylhexyl)dithiophosphoric acid (DETPA) in kerosene, in the presence and absence of alcohols and tri-n-butyl phosphate (TBP) has been studied. Both Ga3+ and Al3+ can be extracted in the form of a neutral complex, MA3, but the distribution coefficient of Ga3+ is the higher by about two orders of magnitude, which can be the basis of the solvent extraction separation of gallium and aluminium. The differences can be explained by the interaction between the sulphur donor atoms of the extractants and the d10 electronic shell of Ga3+ as well as by the lower steric hindrance of ligands co-ordinated to Ga3+.
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