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At least 19 recordsLinked to original sources
PubMed1975

Electrochemical properties of polycyclic compounds studied by the polarographic method in anhydrous systems. II. Polarographic study of carcinogenic nitrogen compounds in dimethylformamide and comparison of half-wave potentials with quantum-chemical calculations of molecular orbitals.

Reduction of half-wave potentials and the mechanism of reduction of 20 polycyclic nitrogen compounds were studied on a dropping-mercury electrode in anhydrous dimethylformamide using tetrabuthylammonium perchlorate as the supporting electrolyte. The measured values of the reducing half-wave potentials of the polycyclic aza-compounds were compared in view of their carcinogenic activity with parental carcinogenic polycyclic hydrocarbons. Electrochemical measurements have confirmed that the size of the shift in reducing potentials towards the more positive values and the decline of the carcinogenic activity generally depend on the number and position of the nitrogen atoms in the molecule of the polycyclic nitrogen compound under study. At the same time, the experimental electrochemical measurements were matched with the results of the quantum-chemical calculations of the molecular orbitals and this showed a good agreement to exist between the values of reducing half-wave potentials obtained by experimental measurement and by calculation.

Aza Compounds↗
PubMed1992

Studies on geranylgeranyl diphosphate synthase from rat liver: specific inhibition by 3-azageranylgeranyl diphosphate.

Geranylgeranyl diphosphate synthase from rat liver was separated from farnesyl diphosphate synthase, the most abundant and widely occurring prenyltransferase, by DEAE-Toyopearl column chromatography. The enzyme catalyzed the formation of E,E,E-geranylgeranyl diphosphate (V) from isopentenyl diphosphate (II) and dimethylallyl diphosphate (I), geranyl diphosphate (III), or farnesyl diphosphate (IV) with relative velocities of 0.09:0.15:1. 3-Azageranylgeranyl diphosphate (VII), designed as a transition-state analog for the geranylgeranyl diphosphate synthase reaction, was synthesized and found to act as a specific inhibitor for this synthase, but not for farnesyl diphosphate synthase. Diphosphate V and its Z,E,E-isomer (VI) also inhibited geranylgeranyl diphosphate synthase, but the effect was not as striking as that of the aza analog VII. Specific inhibition of geranylgeranyl diphosphate synthase by VII was also observed in experiments with 100,000g supernatants of rat brain and liver homogenates which contained isopentenyl diphosphate isomerase and prenyltransferases including farnesyl diphosphate synthase as well as geranylgeranyl diphosphate synthase. For farnesyl:protein transferase from rat brain, however, the aza compound did not show a stronger inhibitory effect than E,E,E-geranylgeranyl diphosphate.

Animals↗
PubMed1977

Dissociation of lipolysis from the levels of cyclic AMP in rat epididymal fat cells.

Two compounds, theophylline and 8-aza-9-furfuryl-adenine (SQ 4665), were found to maximally stimulate lipolysis in preparations of rat epididymal fat cells in the absence of exogenous hormones. Cyclic AMP levels in lipocytes maximally stimulated by either agent alone were unchanged from control levels. In contrast, lipolysis stimulated by either epinephrine alone or in combination with several cyclic nucleotide phosphodiesterase inhibitors correlated well with increases in the levels of cyclic AMP observed. These results suggest the presence of a non-cyclic AMP dependent pathway for the stimulation of lipolysis in rat epididymal fat cells.

Adenine↗
PubMed1991

Some electrochemical characteristics of synthetic analogs of nucleic acid components. IV. 5-Cyano-, 5-carboxy- and 5-azaderivatives, and the effect of this substitution on potential carcinogenicity.

The relation between polarographic reduction, values of half-wave potentials, and the parameter of potential carcinogenicity (tg alpha) was studied in a series of synthetic analogs of natural nucleic acid components modified by different substituents at position 5 of the base. The series included pyrimidine nucleobases (5-cyanouracil, 5-carboxycytosine, 5-azacytosine), ribofuranosyl nucleosides (5-cyanouridine, 5-carboxycytidine, 5-azacytidine) as well as 2'-deoxy-5-azacytidine and 5-carboxy-1-beta-D-arabinosylcytosine. No direct correlation was found between the reducibility of the studied compounds and the parameter of potential carcinogenicity tg alpha since event a slight alteration in the structure of these molecules markedly affected the properties of these compounds.

Aza Compounds↗
PubMed1991

Preparation of potentially bioactive aza and thiaza polycyclic compounds containing a bridgehead nitrogen atom synthesis and antimicrobial activity of some pyrrolo[1,2,3-de]-1,4-benzothiazines.

The synthesis of the 2,3-dihydro-pyrrolo[1,2,3-de]-1,4-benzothiazine 1a and 11b, 12-dihydro-isoquino[1,2-c]-1,4-benzothiazine 8 has been accomplished by using a Bischler type cyclization of the N-(2,2-diethoxyethyl)-3,4-dihydro-2H-1,4-benzothiazines 3a and 3d, respectively. The new compounds 1a and 8 together with the known pyrrolobenzothiazines 1b,c and some their derivatives and intermediates of preparation were tested in vitro for their antimicrobial activity. Compound 1b was the most active against the Gram-positive Bacillus subtilis. Compound 7b showed interesting antifungal activity when tested against Saccharomyces cerevisiae.

Anti-Bacterial Agents↗
PubMedDate not supplied

Antifungal antibiotics from Calcarisporium thermophilum: a new source of 15-azahomosterol derivatives.

Two antifungal metabolites isolated from Calcarisporium thermophilum were identified as 15-azahomosterols related to the compounds previously isolated from Geotrichum flavo-brunneum. By full spectral comparison with authentic 15-aza-24-methylene-D-homocholesta-8,14-dien-3 beta-ol (A 25822 B) from G. flavo-brunneum, the Calcarisporium metabolites were characterized as the 4 alpha-methyl- and 4,4-dimethyl-analogues of A 25822 B. Several minor members of the series were also detected, and tentatively identified by MS analysis. The 15-azahomosterols exhibited good antifungal activity towards Candida parapsiliosis, though the activities were somewhat lower than that of the 4-demethyl derivative A25822 B. Calcarisporium thermophilum is the second microorganism known to synthesize these unusual 15-azahomosterol derivatives.

Antifungal Agents↗