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J Vinsová

Publications and source records attributed to J Vinsová.

7 recordsLinked to original sources
PubMed2004

[Salicylanilides: still a potential antibacterially active group].

The review presents a survey of potential biologically active salicylanilides, focusing particularly on their antibacterial activity. Emergence of bacterial resistance to a large number of antibacterial agents represents a major world-wide problem. On that account, perpetual attention is paid to the preparation of new bioactive antibacterial compounds. Salicylanilides belong to the group of compounds that have shown activity against gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium, the strains representing the most significant problem in clinical practice. In 1998, a new mechanism of their action was proposed. Salicylanilides are inhibitors of two-component regulatory systems in bacteria. Electron-accepting substituents on the salicylic and hydrophobic groups on the anilide ring are most essential for the activity, but other electronic and structural parameters may also play an important role. Our aim, based on SAR analysis, is to develop new active drugs esterified by amino acid and later peptides. Furthermore, analogues carrying the hydroxybenzamide moiety may uncouple oxidative phosphorylation.

Anti-Bacterial Agents↗
PubMed2003

[Biologically active benzoxazoles].

This review presents a survey of preparations and biological activities of substituted benzoxazoles. The structural similarity of benzoxazole derivatives with nucleic bases, such as adenine and guanine, probably allows their easy interaction with biopolymers in the living systems. Consequently, these compounds posses a wide range of biological activities. Their preparation includes cyclocondensation reactions and contractions of ortho-fused heterocycles or their photochemical rearrangement. They are being studied predominantly for their antibacterial, antifungal, antiviral, and antitumor activities, and also as insecticides, herbicides, anthelmintics, histamine antagonists, and fluorescent dyes.

Benzoxazoles↗
PubMed1996

Effect of alaptide, its analogues and oxiracetam on memory for an elevated plus-maze in mice.

In the present study, the elevated plus-maze was used to evaluate memory in female mice. In Experiment 1, the mice retested on day 1, 4 or 7 after the initial session escaped from the open arm into the enclosed arm in a significantly shorter time than those retested on day 10 or 14. Thus, a 10-day inter-session interval was chosen for testing drugs which were expected to enhance memory. In Experiment 2, in the retest performed on day 10, both alaptide (cyclo(L-alanyl-1-amino-1- cyclopentanecarbonyl)) and oxiracetam, given immediately after the 1st session, reduced the transfer latency from the open arm into the enclosed arm as compared with that of the controls. In Experiment 3, a similar effect, i.e., the retention of spatial information, was facilitated by post-session injections of 5 out of 21 alaptide analogues. The new compounds represent the 2,5-piperazinedione derivatives which contain 1-amino-1-cyclo-alkanecarboxylic acid (C3 to C7 ring). The cyclopentane- and cyclohexane-ring was substituted by an alkyl group. In the series with the cycloalkane ring, the importance of the structure of alaptide was confirmed again, which underlines the importance of the cyclopentane ring; the active structures had L-alanine instead of glycine as the second amino acid. Isomers of the cyclohexane series which contained methyl or tert-butyl were most active when the substitution was at position 3. Our results demonstrate that the model of long-term memory can be used to discriminate between closely related chemical structures.

Animals↗
PubMed1991

[The effect of 1-p-bromphenyl-5-mercapto-1,2,3,4-tetrazole (Br FMT) on thyroid gland function in rats].

The effects of the novel potential thyrostatic agent 1-p-bromphenyl-5- mercapto-1,2,3,4-tetrazole (Br-FMT) on the serum levels of thyroxine, thyrotropic hormone (TSH), the content of cyclic adenosine monophosphate (cAMP) in the thyroid gland, the body weight and the weight of the thyroid gland in liver transaminases and the white blood picture in Wistar strain rats were investigated. The effect of Br-FMT was compared with the effect of the well-known thyrostatic agent and goitrogen ethylester of 3-methyl-2-thio-4-imidazoline-1- carboxylic acid, carbimazole (Spofa) and with the control group, which received placebo only. The drugs tested were administered to animals in the dose do 7.5 mumol/animal via a gastric tube for the period of one month. Br-FMT and carbimazole decreased the level of serum thyroxine in a statistically significant manner. The serum level of TSH was evidently decreased after Br-FMT; it was not changed after administration of carbimazole in the given dose. The content of cAMP in the thyroid gland was significantly increased only after carbimazole. The weight of the thyroid gland was not significantly changed in any group under study, though after carbimazole the mean value was higher by a quarter as compared with the control group. The body weight and white blood picture were not significantly changed in all groups under study. ALT and AST values were evidently lower after carbimazole and Br-FMT, most probably due to the hypothyroid state of the animals.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1989

[5-Substituted 3-mercapto-4H-1,2,4-triazoles as a potential thyrostaticagent].

Within the framework of the study of the relationships between the structure and thyreostatic activity of cyclic analogues of thiourea, a series of 5-substituted 3-mercapto-4H-1,2,4-triazoles was prepared in order to answer the question of how the presence of another nitrogen atom in position 1 and the presence of the substituent in position 5 would influence thyreostatic activity. The synthesis was based on 1-acylsubstituted thiosemicarbazides which were cyclized to the pertinent 3-mercapto-4H-1,2,4-triazoles. Furthermore, esters of dicarboxylic acids were used, which with thiosemicarbazide in alcoholate yielded the pertinent mercaptotriazoles. Selected 5-substituted 3-mercapto-4H-1,2,4-triazoles were tested on adult male rats of Wistar strain. The effects of the agents under study on the level of serum thyroxine (T4), total body weight, heart weight, thyroid gland weight, and the number of leucocytes were investigated. The results of the tests show that whereas the presence of nitrogen in position 1 influenced the thyreostatic activity of the agents prepared in an insubstantial manner only, the presence of a substituent in position 5 acts, except a methyl or ethyl group, dystherapeutically, and with the increasing volume of the substituent therapeutic activity disappears regardless of the fact whether an aliphatic or aromatic substituent is concerned.

Animals↗
PubMedDate not supplied

Craniofacial morphology as a marker of predisposition to isolated cleft palate.

The etiology and pathogenesis of isolated cleft palate (CP) is largely unknown. Undoubtedly, bot genetic and environmental factors play a role in initiating this malformation. Although the predictions of the multifactorial threshold model have never been satisfied when subjected to statistical analysis, there is no a priori reason to dismiss the possibility that multiple genes may be segregating in CP families that give rise to specific and predictive phenotypes in the parents of CP offspring. We examined a sample composed of 52 parent pairs whose children were born with CP, as well as 75 normal controls with no family history of CP. Using anthropometric and roentgencephalometric methods, along with discriminant function analysis, we searched for craniofacial variables predictive of parents who were ¿at risk¿ for CP offspring. For fathers of CP children, 32 of the studied variables differed significantly from controls; for mothers of CP children 25 variables differed significantly from controls. These results support the hypothesis that there are characteristic morphometric signs in the craniofacies of the parents of children with CP. To confirm these findings, it will be necessary to prospectively ascertain the incidence of CP in the offspring of ¿at risk¿ parents and ¿not at risk¿ parents from families with and without a history of CP in other family members.

Adult↗