[New pyrimidine compounds with in vitro antimicrobial or antifungal activity].
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Biomedical subjects
Publications and source records attributed to M Ungureanu.
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The antimicrobial and antifungal activity of some 4,4'-bipyridine derivatives were studied. The diffusimetric gelose surface diffusion method with stainless steel cylinders was used to study bacteria and Sabouraud fields for Candida albicans. Comparative analysis of the results led to the following conclusions. Diquaternary salts of 4,4'-bipyridinium possess a remarkable antimicrobial and antifungal activity. The influence of R1 and R2 substitutes in the para or meta position of the benzoylic radical affects selectivity but does not greatly influence activity.
The antimicrobial and antifungical activities of some 1,10-phenanthroline derivatives are described. The test was performed using the diffusimetric method with stainless steel cylinders based on diffusion of the substances on the gelose surface for bacteria and Sabouraud field for Candida Albicans yeast. The comparative analysis of the obtained data leads to the following conclusions concerning the relation between structure and activity
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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.
A feed-forward neural network is used for diagnosis of spastic paralysis. It is a two-layer perceptron and it is able to classify two kinds of myoelectric signal recorded in surface electromyography: the normal EMG and the EMG in the case of spastic paralysis. The myoelectric signal was recorded with a surface electrode pair and sampled at 10 kHz. The EMG activity is stochastic and the instantaneous amplitude distribution for a fixed level of contraction is Gaussian. The signal variance is considered a measure of muscle force. We can describe any kind of this process by the AR model. For a precisely modeling of EMG there are necessary many AR model parameters. In the classification problem we have it is not necessary to use a high order AR model. We find a 4-th order AR model is good enough for this study. The Hopfield algorithm is used to calculate the parameters of the autoregressive model.
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.
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.
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This study presents the synthesis of ten new hydrazides with 1,2,4-triazole support. The structures of the obtained compounds were elucidates by means of the elemental analysis data as well as by IR spectral measurements. The antimicrobial and antifungal actions of this derivates are also tested. The results show that the compounds with the functional group 4-chlore-2-methoxyphenyle are more active.
Nicorandil (N-(2-hydroxy-ethyl)-nicotine amide nitrate), drug recently introduced in therapy, is used as a vasodilator through potassium channel activation. Nicorandil is obtained by treating nicotinic acid chloride hydrochloride with nitro-oxy-ethyl-amine nitrate in an organic solvent. The authors suggest a method that uses ethyl nicotinate as raw material. Thus, the drug can be obtained from indigenous raw materials, at a lower price than the imported ones, with a high purity and a good yield.
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.
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.
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.
In view of studying the pharmacological properties of zinc acexamath a simple and cheap method for the synthesis of acexamic acid by re-evaluating some indigenous raw materials is presented. The conversion of acexamic acid into the corresponding zinc salt is highly efficient by reacting this acid with zinc oxide or zinc carbonate.
Some esters of 7-theophyllinylacetic acid were synthetized, characterized physicochemically and tested for their anti-inflammatory properties. As compared to indomethacin, reference anti-inflammatory drug, all synthetized compounds were less toxic. The anti-inflammatory properties are influenced by the nature of the ester group radicals, the more active having ramified alchils.
Continuing our investigations for obtaining etheric derivatives from the oximes of some carbonylic compounds, five carboxymethylic ethers of some aldoximes were synthetized. Their structure was confirmed by chemical and spectral analyses. The antimicrobial activity of the obtained products towards 6 microorganisms species was determined.
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.