Search

Some novel 1-[2-[[5-(2-furanyl)-4-substituted 4H-1,2,4-triazol-3-yl[thio[ethyl[-2-methyl-5-nitro-1H-imidazoles (3), 1-[3-[[5-(2-furanyl/2-thienyl)-4-substituted 4H-1,2,4-triazol-3-yl[-thio]-2-hydroxypropyl[-2-methyl-5-nitro-1H- imidazoles (5) and 1-[3-[(N,N-disubstituted thiocarbamoyl)-thio[-2-hydroxypropyl]-2-methyl-5-nitro-1H-imidazoles (7) were synthesized and evaluated for in vitro antibacterial and antifungal activity. Some of 5 were found to be effective against bacteria and fungi (minimum inhibitory concentration (MIC) 7.3-125 micrograms/ml), whereas 7 were found to be effective against fungi (MIC 3-25 micrograms/ml).

Electrocardiographic repolarization changes, comprising QT prolongation, are most commonly seen after intracerebral hemorrhage. In this study in patients with intracerebral hemorrhage (ICH), QT dispersion and its daily changes were examined and the relation between QT dispersion and in-hospital mortality assessed. In 28 patients with intracerebral hemorrhage, diagnosed by computerized tomographic scanning, an ECG was obtained on the day of admission to hospital and then serial ECGs were recorded on the following four consecutive days. Blood electrolytes (K, Ca, Mg) were also analysed. The patients with intracerebral hemorrhage were followed until discharge or death (mean 14 +/- 4 days). QT, QT peak, and QT-QT peak dispersion were measured on simultaneous twelve lead electrocardiograms. Also, in 29 healthy subjects as a control group, five consecutive day serial electrocardiograms were recorded. There were no statistically significant differences between the study and control groups in terms of gender and age. During the five days, QT, QT peak, and QT-QTpeak dispersion values were significantly higher in patients with intracerebral hemorrhage than in the control subjects (p < 0.001). There were no statistically significant differences in two patient groups with intracerebral hemorrhage who died and who were discharged in terms of mean QT, QTpeak, and QT-QTpeak dispersion values. In conclusion, QT, QT peak, and QT-QTpeak dispersion values were significantly greater in patients with intracerebral hemorrhage than in the control subjects, but QT, QT peak, and QT-QT peak dispersions were not independent risk factors for in-hospital mortality in patients with intracerebral hemorrhage.

Retinoids reverse the abnormal pattern of keratinization seen in acne vulgaris. Tazarotene is the first of a novel family of topical receptor-selective acetylenic retinoids. This study evaluates the safety and efficacy of topical tazarotene 0.1% and 0.05% gels, in comparison to vehicle gel, applied once daily for 12 weeks, in the treatment of mild-to-moderate facial acne vulgaris. A total of 446 patients with facial acne vulgaris were enrolled, and 375 patients, ranging in age from 14 to 44 years, were evaluable in this multicenter, double-blind, randomized study. In comparison to vehicle gel, treatment with tazarotene 0.1% gel resulted in significantly greater reductions in noninflammatory and total lesion counts at all follow-up visits, and inflammatory lesion counts at Week 12. Tazarotene 0.05% gel resulted in significantly greater reductions in noninflammatory and total lesion counts than vehicle gel at Weeks 8 and 12. At Week 12, treatment success rates were 68% and 51% for tazarotene 0.1% and 0.05%, respectively (40% for vehicle gel). Tazarotene gel was an effective, safe, and generally well-tolerated therapy for the treatment of acne vulgaris.

Background: Topical corticosteroids are often used in the treatment of psoriasis, but long-term use may be associated with serious adverse events such as tachyphylaxis or atrophy of the skin. Tazarotene, a new topical retinoid, has demonstrated significant clinical benefits but can cause mild to moderate local irritation., Objective: We evaluate whether a combination treatment of topical tazarotene and a topical corticosteroid would increase efficacy while reducing the incidence of local adverse events associated with a topical retinoid., Methods: Three hundred patients enrolled in an investigator-masked study were randomly assigned to 1 of 4 treatment groups: tazarotene 0.1% gel in combination with placebo cream, or with a low-, mid-, or high-potency corticosteroid cream, for 12 weeks of treatment and a posttreatment follow-up at week 16., Results: Tazarotene 0.1% gel in combination with a mid- or high-potency corticosteroid, when compared with tazarotene plus placebo cream, achieved significantly greater reductions in scaling, erythema, and overall lesional severity, and a decreased incidence of adverse events., Conclusion: All tazarotene combinations (including tazarotene plus placebo) were highly effective in rapidly reducing the severity of psoriasis. Combining tazarotene with a topical corticosteroid increased efficacy while reducing the incidence of local adverse events.

Pelvic ultrasonography was performed on 75 normal girls. Values were obtained for uterine length, fundal/cervical ratio (FCR), ovarian volume and sex hormones. The resultant data were grouped according to age and pubertal stage (Tanner). For uterine length, FCR and ovarian volume, the data were positively skewed, and the variance increased with age and pubertal stage (p < 0.001). The uterus underwent a regular increase in size and the corpus gradually became larger than the cervix. Uterine length, right ovary volume, FCR and hormones (serum estradiol, follicle-stimulating hormone and luteinizing hormone) showed a correlation with the Tanner score (p < 0.001). Although the correlations were significant, the best correlation was between pubertal stage and serum estradiol level.

In this report, a patient with 100% RCA stenosis and prominent collaterals, in which TI-201 rest/redistribution and Tc-99m tetrofosmin infusion imaging findings were compatible with viable myocardium in contrast to Tc-99m tetrofosmin bolus imaging is presented. Viability was confirmed with improvement of wall motion and perfusion 3 months after revascularization. Infusion of Tc-99m tetrofosmin rather than a bolus injection may be a more reliable technique in the identification of severely ischemic but viable myocardium.

OBJECTIVES: The purpose of the study was to evaluate and compare the immediate and six month follow-up angiographic and clinical outcome of cutting balloon angioplasty and conventional balloon angioplasty in small vessels (less than 3 mm in diameter). METHODS AND RESULTS: Between August 1995 and August 1996 a total of 71 eligible symptomatic patients with angiographically proven significant lesions in their coronary arteries smaller than 3 mm and requiring revascularization, were randomized to receive treatment by either cutting balloon angioplasty (CB) or conventional balloon angioplasty (BA). ÒStand-aloneÓ CB was performed on 51 lesions in 36 patients and BA on 47 lesions in 35 patients. Basic angiographic and clinical characteristics were similar in both groups. The overall procedural success rates for CB and BA groups were 92% and 97%, respectively. The immediate post-procedural minimal luminal diameter, residual stenosis and acute gain were similar in the CB and BA cohorts (1.93 +/- 0.36 mm, 24 +/- 12%, 1.18 +/- 0.45 mm vs. 2.01 +/- 0.34 mm, 22 +/- 9%, 1.26 +/- 0.35 mm, respectively). Total dissection rate and C-F dissections were fewer in the CB group (37%, 6% vs. 51%, 19%, respectively, p < 0.05). Six month follow-up angiographic restenosis rate was lower in the CB group (27% vs. 47%, p < 0.05). We also detected a significant difference of total number of all events at nine month clinical follow up (28% vs. 51%, p < 0.05). CONCLUSION: CB angioplasty can be performed with a comparable success rate to conventional BA in small vessels. Fewer bail-out procedures are needed as CB causes fewer and less severe dissections. There is also a significant reduction in six month restenosis rate. We suggest that CB might be a better option for revascularizing vessels smaller than 3 mm in diameter which are inherently more prone to immediate complications and late restenosis with BA.

Serum fibronectin levels were measured in 63 mothers including 16 healthy normotensive pregnant women, 17 eclamptic women, 16 pre-eclamptic women, and 14 chronic hypertensive patients; as well as their term newborns. There was negative correlation between age-corrected birth weight and mothers' fibronectin levels in the eclamptic and preeclamptic groups, but no significant correlation in the chronic hypertensive group and healthy pregnant women.

Objective: To determine the safety and efficacy of topically applied tazarotene gel in the treatment of mild to moderate psoriatic plaques., Design: Two multicenter, double-blind, randomized studies of 6- and 8-week duration, with an 8-week follow-up in the second study., Setting: Medical center outpatient dermatology services., Participants: One hundred fifty-three adults with 2 bilateral target plaques on the trunk, legs, or arms., Interventions: Vehicle gel or 0.01% and 0.05% tazarotene gel administered twice daily to 45 patients (study A), or 0.05% and 0.1% tazarotene gel administered either once or twice daily to 108 patients (study B)., Main Outcome Measures: Treatment success and plaque elevation, scaling, and erythema vs time., Results: The 0.01% tazarotene gel showed minimal efficacy. Applications of 0.05% and 0.1% tazarotene gels administered once or twice daily, resulted in significant improvements in plaque elevation, scaling, erythema, and overall clinical severity as early as 1 week. Treatment success rates (defined as > 75% improvement from baseline) were 45% with 0.05% tazarotene gel vs 13% with vehicle gel after 6 weeks of treatment (P < .05; study A) and ranged from 48% to 63% with the various tazarotene treatment regimens after 8 weeks of treatment (study B). These improvements were evident at the 8-week follow-up. Treatment-related adverse effects were generally limited to mild or moderate local irritation and were less frequent with the treatment regimen administered once daily., Conclusion: The 0.05% and 0.1% tazarotene gels demonstrated significant efficacy in the treatment of mild to moderate psoriatic plaques that persisted after cessation of treatment.

Background: Topical therapy providing initial improvement and maintenance of effect after treatment of the large majority of patients with limited, mild to moderate psoriasis is not presently available. Previous topical retinoids have generally been either ineffective or too irritating for therapy of psoriasis., Objective: Our purpose was to evaluate a new topical retinoid, tazarotene, in the treatment of stable plaque psoriasis during treatment and posttreatment periods., Methods: In a double-blind manner, 324 patients were randomly selected to receive tazarotene 0.1% or 0.05% gel, or vehicle control, once daily for 12 weeks and were then followed up for 12 weeks after treatment., Results: Of the total, 318 patients could be evaluated. Tazarotene gels were superior (p < 0.05) to vehicle, often as early as treatment week 1, in all efficacy measures: plaque elevation, scaling, and erythema; treatment response; percentage treatment success (patients with > or = 50% improvement); and time to initial success. Efficacy was equivalent on target lesion sites (trunk or limbs and knees or elbows) and overall. A sustained therapeutic effect was observed for 12 weeks after treatment. Tazarotene gel was cosmetically acceptable. There was low systemic absorption, limiting toxicity to local irritation., Conclusion: Once-daily tazarotene was effective and safe as a topical monotherapy for plaque psoriasis, providing rapid reduction of signs and symptoms.

A series of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thiones was synthesized and evaluated for antibacterial and antifungal activity. All of the tested compounds were found active against Staphylococcus aureus and Staphylococcus epidermidis. The compounds were also active against yeast-like fungi and molds where the anticandidal activity of 3a against Candida albicans was superior to the standards miconazole and clotrimazole.

The synthesis of 12 new 4-[(N,N-disubstituted thiocarbamoylthio)acetamido]antipyrines and their antifungal activity are reported. Of these compounds, only 3e, showed good antifungal activity against C. tropicalis KUEN 1021, C. krusei KUEN 1001, C. stellatoidea KUEN 1018, C. pseudotropicalis KUEN 1012, C. albicans ATCC 10231 when compared with clotrimazole and miconazole (MIC = 12.5 micrograms/ml).

Background: Oral retinoids have been widely used in psoriasis, but topical forms have been ineffective or irritating., Objective: Our purpose was to determine the clinical and molecular effects of a new topical retinoid, AGN 190168, on psoriasis., Methods: Seven patients with psoriasis were treated for 2 weeks with topical retinoid and 2 weeks with vehicle. Two control subjects with psoriasis were treated for 2 weeks with vehicle alone. Biopsy specimens from normal skin as well as from untreated and treated psoriatic lesions were compared by immunohistochemical analysis. Differentiation and inflammatory markers were studied., Results: Clinical improvement was seen in all seven patients after 2 weeks of treatment. Improvement was still present, but not significant, after 2 additional weeks of vehicle application. Histologic examination showed a return to a more normal morphology in four of seven biopsy specimens, which correlated with filaggrin expression. There was a diminution in the precocious expression of keratinocyte transglutaminase, keratin 16, and involucrin, as well as a decrease in epidermal growth factor receptor and in the number of cells expressing intercellular adhesion molecule type 1 and HLA-DR., Conclusion: Clinical and histologic improvements were seen in psoriasis in association with the topical application of AGN 190168 at 2 weeks, including decreased inflammation and restoration of normal epidermal differentiation. Small patient numbers and the possibility that the changes were related to clinical improvement alone and not the topical agent preclude definitive conclusions.

Seventy patients with tinea cruris or tinea corporis were treated with naftifine cream 1% or vehicle once daily for 4 weeks in this double-blind, randomized study. After two weeks, the patients using naftifine had a significantly higher mycologic cure rate than the vehicle-treated patients (79% vs. 31%, p less than 0.001), and they showed significantly better resolution of signs and symptoms. Statistically significantly differences favoring naftifine over its vehicle were found throughout the treatment period and 2 weeks posttreatment.