In vitro aldose reductase inhibitory activity of substituted N-benzenesulfonylglycine derivatives.

A number of N-benzenesulfonylglycines, alanines, sarcosine, and prolines, which contain the minimum pharmacophore moieties necessary for aldose reductase inhibitory activity, were prepared and tested in the rat lens assay. In this assay, the benzenesulfonylglycines are considerably more potent than the corresponding alanine and sarcosine derivatives which, in turn, are more active than the proline analogues. Of the monosubstituted benzenesulfonylglycines, the 2-nitro and 4-amino derivatives were most active with 50% inhibitory concentration (IC50) values of 13 and 16 microM, respectively. The most potent derivatives evaluated were the beta- and alpha-naphthylenesulfonylglycines with IC50 values of 0.4 and 1.3 microM, respectively. The structure-activity data obtained from evaluation of the benzenesulfonylamino acids suggests that the aromatic ring and ring substituents, as well as the sulfonamide group and carboxylate moiety, all contribute to the inhibitory potency through direct interaction with complimentary binding sites present on aldose reductase.

Exercise training in black adolescents: changes in blood lipids and Vo2max.

The purpose of this investigation was to evaluate the effects of a 15-week exercise training program on cardiovascular and blood lipid variables in black adolescents. Subjects consisted of black males with 12 of these participating in an exercise conditioning program and 5 designated as the control group participating in a team sports program. The mean +/- SD age was 12.8 +/- 0.97 yrs. Training for the exercise group was conducted 5 d.wk-1 for 15 weeks (weight training 2 d.wk-1 and aerobic training 3 d.wk-1). The following mean +/- SD significant changes were found for pre- to post-training for the exercise group (P < 0.05) with no significant change for controls: high density lipoprotein cholesterol (HDL-C) 1.11 +/- 0.18 to 1.28 +/- 0.17 (mmol.l-1), low density lipoprotein cholesterol (LDL-C) 2.73 +/- 0.74 to 2.41 +/- 0.81 (mmol.l-1), maximal oxygen uptake (VO2max) 43.7 +/- 9.4 to 48.2 +/- 9.7 (ml.kg-1.min-1), and maximal ventilation (VE max) 70.59 +/- 16.8 to 80.93 +/- 14.6 (L.min-1). In addition, no significant changes were found for blood pressure or other blood lipid parameters for either group. Results of this study show that exercise training can favorably alter blood lipid and VO2max values. Therefore, a vigorous exercise training program for young black males can favorably affect their cardiovascular risk profile.

Liquid chromatographic determination of the enantiomeric composition of amphetamine and related drugs by diastereomeric derivatization.

A procedure is described for the derivatization of amphetamine and methamphetamine enantiomers with 4-nitrophenylsulfonyl-(S)-prolyl chloride. The resulting diastereomeric amphetamine derivatives were resolved by a reversed-phase procedure. The derivatization yield was maximized in the 95% range using a five-fold molar excess of the chiral derivatizing agent and an approximate 18 to 1 ratio of base (NaHCO3) to total acid generated in the reaction.

Liquid chromatographic measurement of hydrophobicity constants for N-arylsulfonylglycine aldose reductase inhibitors.

The hydrophobicity constants for a series of aldose reductase inhibitors (ARIs) are determined by reversed-phase liquid chromatography. A series of reference compounds consisting of 23 barbituric acid derivatives are separated on two phenylsilica stationary phases over a range of methanol concentrations (30-80%) in 0.05 M phosphate buffer. Linear regression analysis of the measured log k' data is used to estimate the capacity factor in 100% water (log k'w) for each compound. The log k'w values are regressed against the shake-flask-measured 1-octanol-water partition coefficients, producing a correlation of 0.953. The same procedure is then used to estimate the log k'w values for a large group of ARIs and their log P values, calculated from the established relationship between log k'w and log P from the reference compounds. An initial analysis of the aldose reductase inhibitory activity of these compounds as a function of hydrophobicity alone fails to reveal a clear relationship, demonstrating the need for a multivariant approach for quantitative structure-activity analysis in this series of compounds.

Iron status in women aerobic dance instructors.

This investigation evaluated the iron and nutritional status of 12 highly trained aerobic dance instructors who did not take iron supplements (ANS) and 8 who did (AS). A control group (C) consisted of 10 age matched controls. The aerobic instructors had exercised for approximately 3.8 days/wk, 56 min/session for the past 7 yrs. There were no significant differences among groups for energy intake, carbohydrate, protein, fat, nonheme iron, heme iron, or total iron intake (excluding supplemental iron). But both exercise groups had lower ferritin values than the control group. There was also a significant difference in mean cell volume (MCV), with both exercise groups having greater values than the control group. There were no differences among groups for serum iron, total iron binding capacity, transferrin saturation, hematocrit, or hemoglobin. One in three aerobic dance instructors had serum ferritin values below 12 micrograms.L-1. Results indicate that women exercise leaders have iron profiles that are similar to other groups of female athletes. The increased MCV values suggest runners' macrocytosis or an exercise induced macrocytosis.