[Antimicrobial activity of new pyridazine derivatives]. / Activité antimicrobienne de nouveaux dérivés de la pyridazine.

Continuing the investigations concerning synthesis-structure-biological activity in the pyridazine series, the results of the antimicrobial and antifungal tests of some new pyridazinium compounds are presented. The test was performed using the diffusimetric method with rustles steel cylinders based on the diffusion of the tested substances on the gelose surface. The comparative analysis of the obtained data leads to the following conclusions concerning the relation between structure and activity in the pyridazine series: 1. The cis-isomers are always more active comparatively with similar trans- isomers: 2. In the pyrrolopyridazine series we remark that the saturated or partial saturated compounds have always a stronger activity as the related aromatics derivatives. We also noticed that the saturated, partial saturated and aromatic compounds have different selectivity. Thus, the saturated are more active on the Pseudomonas aeruginosa and Candida albicans, the partial saturated are more active on the Staphylococcus aureus and Bacillus subtilis while the aromatic compounds are active on the Bacillus subtilis. 3. The influence of the Y-substitutes of para position of benzoylic radical and the substitutes of pyrrolo ring is not decisive towards activity, these affecting especially the selectivity.

[Experimental data on pharmacological effects of new phenothiazine derivatives]. / Données expérimentales concernant les effets pharmacologiques de quelques nouveaux dérivés phénothiaziniques.

A variety of triazoles and thiadiazoles linked to the N-atom of the phenothiazine through a two carbon atoms chain have been submitted to preliminary toxicological screening (DL50 and DMT). Two derivatives have been selected for the specific pharmacological evaluation. It has been noted a diminution of the exploratory capacity without the muscle tonus, the balance and the capacity of becoming normal again of the tested animals (mice and rats) being affected.

[New derivatives of 1-methyl-phthalazine with antimicrobial and fungistatic action]. / Nouveaux dérivés de la 1-méthyl-phtalazine doués d'activités antimicrobiennes et fongistatiques.

In this paper we present the antimicrobial and antifungical action of some new salts of 1-methyl-phtalaziniums and their corresponding ylids. We also present conclusions concerning the relation between structure and biological activity. The test was performed using the diffusimetric method with rustless steel cylinders based on the diffusion on the tested substances on gelose surface. The salts of 1-methyl-phtalaziniums are always more active comparatively than their corresponding ylids. All the compounds but not all derivatives are more active on the Candida albicans.

[Antimicrobial activity of some derivatives of pyrimidine]. / Activité antimicrobienne de quelques dérivés de la pyrimidine.

In this paper the authors present the antimicrobial and antifungical tests of some new 3-methylpyrimidine compounds. The test was performed using the diffusimetric method with rustlessteel cylinders based on the diffusion of the tested substances on the gelose surface. The comparative analysis of the obtained data leads to the following conclusions concerning the relation between structure and biological activity in the pyrimidine series: 1. The pyrimidinium ylides are less active comparatively with the corresponding salts. That means that the zwitter ionic structure did not favour the activity. 2. Comparative with the corresponding pyridazine(1,2-diazine) derivatives, the pyrimidine(1,3-diazine) compounds are more active. The increase of activity of the pyrimidine compounds could be attributed of the influence of the pyrimidine ring. 3. The most active pyrimidine compound which is tested is that one in which radical R is an amide group. 4. In the case when the radical R is a phenyl ring, the substitute from para position of benzoylic radical does not appear decisive towards activity, these affecting especially the selectivity.

[Amphoteric ion intermediates in the pyrazine series. II. The action of p-nitrophenacyl bromide on pyrazine]. / Intermediari amfionici din seria pirazinei.II. Actiunea bromurii de p-nitro-fenacil asupra pirazinei.

Continuing to present the results of the investigations carried out on the amphoteric ions intermediates of the N-heteroatomic system with 2 natrium atoms in positions 1, 4, new pyrasine derivatives synthetized with p-nitro-phenacyl bromide are described. The observations on their antimicrobial and antiyeast activities is discussed.

[New pyridazine compounds with possible physiological action]. / Noi compusi piridazinici cu eventuala actiune fiziologica.

The methods of obtaining and the physicochemical and spectral characterization of eight new pyridazine derivatives are presented. Thus, the reaction of chlorine-hydrazino-pyridazine with pyruvic and alpha-ketoglutaric acids resulted in the corresponding hydrazones. Using the indications in the literature the tetrazolic, triazolic, pyrazolonic and phenyl-thiocarbazidic derivatives of hydrazino-pyridazine were synthetized. The structure of the new compounds was confirmed by carbon, hydrogen and nitrogen analyses and spectral ones in infrared.

[Ilide derivatives of pyridazines with biological activity]. / Derivati ilidici ai unor piridazine cu activitate biologica.

Continuing the investigations on the synthesis and pharmacodynamic action of some pyridaziniu-ilides, this paper presents the results of the preliminary investigations on the antimicrobial activity of the synthetized products. Their action against Staphylococcus aureus Oxford and the anti-yeast action of the cycloimonium salts is underlined.

[Phthalazinilides. The action of ethyl bromopyruvate on phthalazine]. / Ftalaziniu-ilide. Actiunea brompiruvatului de etil asupra ftalazinei.

Our investigation for obtaining carbon-nitrogen stable ilides continued by the synthesis of new phthalazinic derivatives by the action of ethyl brompyruvate. The structure of the obtained products was confirmed by chemical and spectral analyses. The results regarding their antimicrobial action are also presented.

[Synthesis and physicochemical and biological characteristics of phthalazine derivatives]. / Sinteza si caracterizarea fizico-chimica si biologica a unor derivati de ftalazina.

Further studies in view of obtaining new stable phtalasiniuilides present the synthesis and physico-chemical and biological characterization of certain derivatives obtained through the action of p-phenyl-phenacyl and p-nitro-phenacyl bromides upon R-phtalasine. The structure of the new products was confirmed by physicochemical and spectral analyses. The preliminary biological tests showed a moderate antimicrobial activity of certain studies compounds.

[The synthesis and biological activity of new disubstituted carbanion ylides from pyridazine]. / Synthèse et activité biologique de quelques nouveaux pyridazinum--ylures à carbanion disubstitues.

Continuing the investigations in view obtaining new carbon-nitrogen stable dissiniu-ilydes, were obtained new 3-phenyle-pyridaziniu-ylides carbanion disubstituted. The antimicrobial and antifungus action of the products VIa, VIb, VIIa, VIIb and VIIc also studied.

[Phtalazinium lures (VIII). Action of p-nitrophenacyl bromide on phtalazine]. / Phtalazinium-ylures (VIII). Action du bromure de p. nitrophénacyle sur la phtalazine.

Continuing our investigations for obtaining stable diazinium-ylures, the conditions of obtaining and reactivity of p-nitrophenacyl-phtalazinium methylides were studied. This ylure leads by 3+2 dipolar cycloaddition with dimethyl acetylenedicarboxylate and N-phenyl-malein-ymide to the respective cycloadductions. The synthetized compounds were tested biologically.

[The synthesis of new pyrrolidone derivatives with psychotropic action]. / Sinteza unor noi derivati pirolidonici cu actiune psihotropa.

The synthesis of ten new heterocyclic compounds obtained by the addition of pyrrolidone to heterocumulenes and its condensation or of its sodic derivative with acid chlorides is presented. The synthetized pyrolidonic derivatives were subjected to a preliminary study for determining their possible psychotropic action. The pharmacological screening evidenced a significant hypothermisante and neurodynamic-nootropic action of some synthetized compounds.

[Studies regarding the fixing of the zinc from ADH through some azopyrazolone]. / Cercetari privind modul de fixare a zincului din ADH prin intermediul unor azopirazolone.

The mechanism of reaction-between the zinc atom of alcohol dehydrogenase and 6 pyrazolone and azopyrazolone compounds, type 1-(4'-carboxyphenyl)-3-methyl-4(1"azo-4"-ethoxy-phenyl)-5-pyrazolone, synthetized by the authors, is studied. For elucidating the "in vivo" phenomenon, the complexes of these compounds were synthetized with zinc atoms, the IR specters and quantitative chemical analyses being followed. Based on these, the possibilities of complexing the zinc from the ADH molecule by these compounds are discussed.

[Pyridazinilides (XIV). The action of p-phenyl-phenacyl bromide on 3-phenyl-pyridazine]. / Piridaziniu-ilide (XIV). Actiunea bromurii de p-fenil-fenacil asupra 3-fenil-piridazinei.

This time the synthesis of some new derivatives obtained by the quaternary substitution of one of the heterocyclic nitrogen atoms and by reactions of dipolar cycloaddition is presented. The results of the tests on their antimicrobial and antiinflammatory actions are discussed.