Timing of analog research in medicinal chemistry.

Analog research plays an important role in medicinal chemistry. Having identified a new target in molecular biology many similar lead compounds are synthesized resulting in closely related products on the market. Another approach is the further optimising of an existing drug in order to improve on the original. In some cases these two approaches overlap. The question of timing and the importance of analog research are analyzed in this paper.

4-(1-Naphthylamino)-piperidines as inhibitors of lipid peroxidation.

Some analogues of (+/-)-N-methyl-N-¿1-[3-(4-fluorophenoxy)-2-hydroxy-propyl]-piperidin+ ++-4-yl¿ benzothiazol-2-amine (sabeluzole, CAS 104383-17-7), a series of 4-(l-naphthylamino)-piperidines (1a-1h), are potent inhibitors of both NADPH- and Fe(2+)-dependent lipid peroxidation (IC50 < 10 mumol/1). It was demonstrated that the naphthylaminopiperidine moiety is responsible for this effect due to its antioxidant property, verified by cyclic voltammetric studies.

Inhibitors of lipid peroxidation among new pyrimido[1',6':1,2]pyrido[3,4-b]indoles.

A series of potent inhibitors of NADPH- and Fe(2+)-dependent lipid peroxidation has been found among new pyrimido[1'6':1,2]pyrido[3,4-b]indole derivatives. According to preliminary structure-activity relationship analysis the saturated pyrimidine moiety was responsible for this effect. Some members of this family were effective in a bilateral carotid occlusion model in mice, and some derivatives showed protective effect in a mouse head injury model.

A survey on operating conditions and quality of commercial frying fats in Hungary.

An extensive survey on commercial frying fats was conducted in Budapest. It was based on sample collection, analysis and questionnaires filled in with each sample. Frying fats and oils were collected from restaurants, fast-food services and public catering facilities. The quality of samples was assessed by determining their polar components. An evaluation of questionnaires containing over 20 questions yielded detailed information on the usage of fats as well as the fryer operators' habits of conducting frying processes and their knowledge on the subject. The survey consisted of two periods. During the first period 252 samples were collected at random. Quality assessment indicated that 53.6% of all samples was of good quality (with concentrations of polar materials below 25%) while the rest were at the discard point or deteriorated. The second part of the survey was aimed at a recheck of the places where fat had been found deteriorated. Second samples were obtained from 53 establishments. The results showed an improvement both in operating conditions and quality of frying fats. Based on the results, the necessity of instructing fryer operators and introducing regulations and routine quality testings of frying fats became obvious.

Effect of soya consumption on hepatic monooxygenase enzyme system and some lipid parameters in rats.

Young male rats were fed with diets containing Hungarian soya products (extruded or granulated soya preparates) as the only source of protein for four weeks. The weight gain of the animals, the cholesterol and triglyceride content of liver and the activity of the hepatic monooxygenase system were studied. 20% soya protein in the diet (either from extruded or from granulated soya products) supplemented with sulphur containing amino acids met the protein requirement of the young growing rats. In a separate experiment the protein depletion-repletion method was used to investigate the effect of Purina 500 E soya protein isolate on the above mentioned parameters. The results indicate that diets containing 20% soya protein are satisfactory for the regeneration of the protein depleted animals.

Fatty acid composition of human milk and milk-based formulas in Hungary.

Fatty acid composition of breast milk from 250 Hungarian women being 1, 3 and 6 months post partum was studied. It was shown that the fatty acid composition of mature breast milk does not vary greatly with the length of lactation. Data from women with different education levels and places of residence were found similar, suggesting similarities in the dietary habits of Hungarian women. Fatty acid levels in human milk did not show significant seasonal variation. The content of linoleic acid (expressed as g/l and percent of total energy) was calculated in relation to the length of lactation. Fatty acid composition of Hungarian milk-based formulas (Robebi A, Robebi B and Linolac) was also studied and compared to the mean composition of milk from 250 mothers. The results indicated differences in the contents of most saturated and unsaturated fatty acids and confirmed the finding that even the most carefully adapted formulas cannot substitute human milk.

Decrease in essential fatty acid content of edible fats during the frying process.

Degradation of sunflower oil, rapeseed oil, and lard during the frying operation was investigated by studying the loss of essential fatty acids compared to the accumulation of decomposition products. Linoleic and/or linolenic acid concentration was measured by GLC, and for detecting decomposition products determination of polymer content by GPC was chosen. Twelve laboratory experiments with different heating or frying conditions were run aimed at modelling practice and studying the effects of certain factors. The results indicated that loss of essential fatty acids being a parallel process to the accumulation of breakdown products is suitable both for detecting the decrease in nutritive value and for quality assessment of used frying fats. It was also found that the rate of deterioration is considerably affected by the nature of fat and the frying parameters. Study of the relationship between polymer content and the decrease in essential fatty acid concentration (using data from 110 samples) showed that high, linear correlation depending on the nature of fat can be found. Correlation coefficients and equations of regression lines were calculated.