[Polyphenol compounds from Hamamelis virginiana L]. / Polyfenolické obsahové látky z Hamamelis virginiana L.

Two phenolic acids and two flavone aglycones were isolated from the aboveground part of Hamamelis virginiana L. and identified with the use of thin-layer chromatography, melting points, and spectroscopic methods as gallic acid, ethyl gallate, quercetin, and kaempferol.

[Preparation and antiinflammatory activity of selected aqua-(aryloxyacetate) zinc complexes]. / Príprava a protizápalová aktivita vybraných akva-(aryloxyacetáto)zinocnatých komplexov.

Mononuclear aqua(aryloxyacetato)zinc(II) complexes of the composition [Zn(H2O)2(ROCH2COO)2] (R = phenyl, o-, m-, p-tolyl) were prepared as potential anti-inflammatory agents. The results of elemental analysis and parameters of IR spectra allow to classify the above-mentioned compounds to the group of carboxylatozinc(II) complexes with a distorted octahedral structure. They were assayed in rat paw carrageenan-induced edema and antiedematous effects were compared to those of free acids. Salicylic acid and its zinc(II) and copper(II) salts were used as the standards of comparison. All compounds were administered i.p. in a single dose of 50 mumol/kg body weight (calculated for the carboxylate fragment). In general, the zinc(II) complexes tested were clearly more effective (expressed as a mean edema reduction of 58-70-68-59%), including zinc(II) salicylate dihydrate (64%), than the uncomplexed acids (37-26-50-48%). Copper(II) salicylate tetrahydrate (60%) and salicylic acid (57%) exhibited comparable effects under the same conditions. The observed activities of the complexes are discussed in relation to their structures as well as to the coordination-chemical properties of the acidoligands under study.

[Preparation and anticonvulsant activity of new potential beta-adrenoreceptor blockers]. / Príprava a antikonvulzívna aktivita nových potenciálnych blokátorov beta-adrenoreceptorov.

Within the framework of a structure-effect relationships study in a group of new beta-adrenoreceptor blockers, a series of new derivatives derived from p-hydroxyacetophenone with modifications in the basic moiety of the side chain was prepared. The initial p-hydroxyacetophenone prepared by Fries rearrangement of phenylacetate in a reaction with 2-(chloromethyl)oxirane yields 1-[4-(2-oxiranylmetoxy)phenyl]-1-etanone, which combines with the appropriate amines to produce final substances. They were isolated either in the form of free bases, or salts with fumaric acid. Their structure was confirmed by interpretations of the IR, 1H-NMR and 13C-NMR-spectra. Within the framework of pharmacological evaluation of the prepared agents, the anticonvulsive effect as a protective effect against pentetrazole spasms was examined. The results of the evaluation were compared with the values of their distribution coefficients.

[Antimicrobial activity of (N-salicylidene-DL-aspartate- and (N-salicylidene-L-asparaginate)-copper complexes with pyrazole-type ligands]. / Antimikróbna aktivita (N-salicylidén-DL-aspartáto)- a (N-salicylidén-L-asparagináto) mednatých komplexov s ligandmi pyrazolového typu.

By a reaction of salicylaldehyde (Scl) with the corresponding amino acids and by the next complexation reaction of the formed Schiff bases with Cu2+ ions in an aqueous-alcoholic medium, aqua (N-salicylideneaminoalkanoato)copper(II) complex chelates of the composition Cu(Scl-DL-Asp(2-)) (H2O)2, Ip and Cu(Scl-L-Asn(2-)(H2O), In were prepared. The monodiazole complexes with pyrazole IIp and IIn (as monohydrate) as well as with 3,5-dimethylpyrazole IIIp a IIIn were prepared by replacing the molecule of H2O in the parent aquacomplexes with the diazoles under the same reaction conditions. Using a routine dilution micromethod, the antimicrobial activity of the prepared complexes and free diazoles was tested against Staphylococcus aureus, Escherichia coli and Candida albicans. Only a significant antistaphylococcus activity was found (highest for the complex IIn; MIC = 39 micrograms/cm3). All chelates (Ip,n-IIIp,n) were more effective (MIC = 39-156 micrograms/cm3) than both pyrazole (312 micrograms/cm3)and 3,5-dimethylpyrazole (625 micrograms/cm3) alone. The relationship between the coordination-chemical properties and the biological effects of the complexes studied is discussed.

[Royleanones in the roots of Salvia officinalis L. of domestic provenance and their antimicrobial activity]. / Royleanóny v koreni Salvia officinalis L. domácej proveniencie a ich antimikróbna aktivita.

The reported investigation of the constituents of the petroleum ether extract of the root of Salvia officinalis L. confirmed the presence of the following diterpene quinones: 12.hydroxy-8, 12-abietadiene-11, 14-dione (royleanone), 7 alpha, 12-dihydroxy-8.12-abistadiene-11-14-dione (horminone) and 7 alpha-acetoxy-12-hydroxy-8, 12-abietadiene-11,14-dione (7-O-acetylhorminone). The compounds were identified on the basic of the interpretation of results of spectral analysis. Isolated royleanones show antimicrobial activity against gram-positive bacteria (Staphylococcus aureus). A study of abietate diterpenoids in the root of Salvia officinalis L. of Slovak provenance has been performed for the first time.

Model compounds in elucidating the structural basis of HIV retrovirus activity. Synthesis of trisodium O-monoalkyl- and O-monoaryldiphosphates.

Trisodium salts of O-methyl, O-butyl, O-phenyl, and O-(4-nitrophenyl)diphosphonic acids were prepared by reaction of sodium dimethylamido-O-(2-cyanoethyl)phosphate with O-alkyl-, and O-arylphosphonic acid. In an effort to obtain anhydrous salts of the acids, besides the conventional method using aqueous sodium hydroxide, another procedure involving reaction, of sodium methoxide in methanol was also used. The structure of the final compounds was confirmed by IR, 1H NMR and 31P NMR spectra. The prepared salts of monosubstituted diphosphonic acids are used as model compounds in studying antiviral and cytostatic activity of phosphorous derivatives of purine and pyrimidine bases.