The lysine pathway as a target for a new genera of synthetic antibacterial antibiotics?

Unsaturated analogues of diaminopimelic acid have been synthesized. The amino acids were designed so that they would be reversible or irreversible inhibitors of both of the two last enzymes of the lysine pathway. The compounds were tested with meso-diaminopimelate decarboxylase. trans-3,4-Didehydrodiaminopimelic acid (2) was found to be the most potent inhibitor. The antibacterial activities did not correlate with enzyme inhibiting activities. 4-Methylenediaminopimelic acid 4 showed strong antibacterial properties. It is suggested that L,L-diaminopimelate epimerase could be the target enzyme.

A long-term study of penfluridol in chronic schizophrenia.

Penfluridol, a member of the novel diphenylbutylpiperidine class of antipsychotic drugs, is the first long-acting oral neuroleptic. The population of the present study consisted of 24 chronic schizophrenic patients (14 males, ten females) whose treatment with penfluridol was initiated in our previous open/double-blind trial lasting 32 weeks 1; mean age was 42.2 years and mean duration of illness, 15.4 years. During one additional year in an uncontrolled clinical study, penfluridol in the form of 20-mg capsuent procedures included BPRS, CGI, NOSIE, vital signs, and laboratory measurements. During this long-term treatment with penfluridol, the scores of a cluster of BPRS items that included emotional withdrawal, conceptual disorganization, motor retardation, uncooperativeness, and blunted affect showed a progressively significant improvement. This indicated that the Bleulerian primary symptoms in chronic schizophrenics can be improved by the long-term administration of this long-acting neuropleptic with concomitant betterment of social adaptation and activity. The percentage of failure was very low (four patients) and was marked by instability of psychopathology with periods of excitation. The incidence of extrapyramidal reactions necessitating the administration of an antiparkinsonian drug during the length of trial was 35 per cent. No serious effects nor significant laboratory test changes were observed.

A supermarket cardiovascular screening program: analysis of participants' solicitation of follow-up care.

We conducted a cardiovascular screening program in 54 supermarkets in the province of Québec, Canada to determine cardiovascular risk factors, including total cholesterol, blood pressure, tobacco use, height, weight, and physical activity levels. A 10-minute debriefing counseling session followed. Of the 3,432 screening participants 18-74 years of age, 2,420 participated in a nutrition study, consisting of answering a brief questionnaire before the screening. Three months after the screening, 1,293 individuals returned the posttest nutrition questionnaire sent to them by mail. We report follow-up care activity for low-risk and high-risk individuals for respondents of the posttest nutrition questionnaire. Overall, 53% of respondents reported seeing a physician within three months after the screening to discuss their blood cholesterol or blood pressure results, and the percentage ranged from 25% for individuals with normal cholesterol (< or = 199 mg/dL) and normal blood pressure (< 140/90 mm Hg) to 83% for individuals with high cholesterol (> or = 240 mg/dL) and high blood pressure (> or = 140/90 mm Hg). Respondents who saw a physician following the screening were more likely to be (1) those on medication at the time of the screening for high blood cholesterol and high blood pressure, (2) older individuals, (3) those found to have high blood cholesterol and high blood pressure values during the screening, (4) women, and (5) individuals with a lower level of education. Seventy-nine percent identified as having high blood cholesterol during the screening reported that their blood cholesterol was remeasured. The majority of high-risk participants and their physicians took appropriate follow-up action.(ABSTRACT TRUNCATED AT 250 WORDS)

Health risk appraisal in an occupational setting and its impact on exercise behavior.

The aim of this study was to evaluate the impact of a health risk appraisal (HRA) activity on exercise intention and behavior modification. In a mixed experimental and quasiexperimental design, three groups of subjects were formed: (1) preintervention, (2) postintervention, and (3) control. In the experimental design, the results showed that the employees in the postintervention group had, immediately after the HRA activity, an increased intention to exercise regularly compared with the employees in the preintervention group. According to the quasiexperimental design, the employees exposed to the HRA activity did not, 2 months later, report regular exercise behavior that differed from that of the employees in the comparison group. It is suggested that an HRA activity should be supplemented with regular additional interventions over a given period of time to be successful in supporting the process of translating exercise intention into behavior.

Synthesis of pseudotrisaccharides related to ribostamycin.

The three protected sisamine derivatives 2i, 2j and 3, with a free 5-hydroxyl group, have been synthesized. Glycosylation at the 5 position with various pentofuranose derivatives yielded after deprotection of the 6a approximately i ribostamycin related aminoglycoside. These pseudotrisaccharides showed only low antibacterial activities with respect to the parent compounds.

Synthesis of sisamine and of pseudodisaccharide analogues.

Lividamine and paromamine were converted into two key intermediate ethylenic aldehydes 10a and 10b. Reductive amination of the two aldehydes yielded the protected sisamine 11a and the three analogs 11b, 12a and 12b. These four derivatives were deprotected to yield the four pseudodisaccharides 1a, 1b, 2a and 2b which were less active in vitro than neamine against Escherichia coli ATCC 9637 and Staphylococcus aureus 209P.

Changes in knowledge and food behaviour following a screening program held in a supermarket.

We examined the relationship between knowledge, health beliefs and dietary behaviours of participants in a supermarket cardiovascular screening program, the conceptual framework for which was the Health Belief Model. 3,432 individuals aged 18-74 participated in the screening program conducted in 54 supermarkets in Montreal and Quebec. This program identified participants' risk for cardiovascular disease by measuring total serum cholesterol, blood pressure, height, weight, level of physical activity, and tobacco use. A ten-minute debriefing counselling session interpreted risk factors and recommended follow-up. 70% (n = 2,420) also completed a nutrition questionnaire on knowledge, health beliefs, and frequency of consumption of high fat foods. Respondents increased their knowledge and reduced the frequency of consumption of high-fat foods following the screening program (p < or = 0.05), particularly individuals with higher blood cholesterol levels, high blood pressure, and women.

Epidemiology of tardive dyskinesia Part I.

We have performed an epidemiological study concerning tardive dyskinesia on a sample of 332 chronic schizophrenic patients (142 males and 190 females, mean age 48.6 years, mean duration of neuroleptic treatment 14.5 years). We could conclude that the age of patients at the time of assessment procedures is the most important variable. The prevalence of tardive dyskinesia was significantly higher in the older population. The significance of an insidious beginning of the illness might be only secondary to the highly significant role of the age. Other factors, such as sex, type of schizophrenia, initial syndrome, present psychic state, organic syndromes and neuroleptic-induced extrapyramidal syndrome, do not seen to play a role in the prevalence of tardive dyskinesia.

Epidemiology of tardive dyskinesia. Part II.

In the part II of an epidemiological study on tardive dyskinesia performed on the same sample of 332 chronic schizophrenic patients (142 males and 190 females), the authors come to the conclusion that the prevalence of tardive dyskinesia is significantly higher if the mean age was higher at the beginning of treatment with sedative or incisive neuroleptics, their combinations (cocktails) and added antiparkinsonian drugs. Age seems to be the most important factor in the prevalence of tardive dyskinesia. The mean longer duration of "incisive" free intervals significantly decreases the prevalence of tardive dyskinesia. Other factors analysed in our sample, especially the total amount of neuroleptics administered, the type of neuroleptics and the mean duration of neuroleptic treatment, do not play a significant role in the prevalence of tardive dyskinesia.