Medicinal Chemistry: Enantioselectivity of Some 1-(Benzofuran-2-yl)-1-(1-H-imidazol-1-yl) Alkanes as Inhibitors of P450Arom

The low stereospecificity of the enantiomers of 1-[(benzofuran-2-yl)-4-chlorophenyl-methyl]imidazole ( 6 , R = H, R' = 4′-Cl) and the corresponding 4-fluoro compound as inhibitors of aromatase (P450_Arom) has been explored using 1-(5,7-dichlorobenzofuran-2-yl)-1-(1H-imidaz-1-yl)ethane ( 7 , R₁=R₂ = Cl, R = CH₃), -propane ( 7 , R₁=R₂ = Cl, R = C₂H₅), and the corresponding 5,7-dibromo compounds resolved as their dibenzoyl-D (or -L) tartrates. Low enantioselectivity ratios of 4.8 (5,7-diCl) and 12.6 (5,7-diBr) were shown for the ethanes. The values for the corresponding propanes were 8.3 and 5.2, respectively, and for these compounds the stereoselectivity was reversed.     

Are Retinal Microvascular Caliber Changes Associated with Severity of Coronary Artery Disease in Symptomatic Cardiac Patients?

Objectives: Recent population‐based studies have shown that retinal vascular caliber may predict the risk of clinical coronary artery disease (CAD) events. Whether this association is related to macro‐ or microvascular mechanisms remains unknown. We investigated the relationship of retinal vascular caliber with severity and extent of CAD in symptomatic cardiac patients. Materials and Methods: Overall, 98 patients attending diagnostic coronary angiography were recruited. Coronary angiography was used to assess for the severity and extent of CAD. Digital retinal photography was performed immediately prior to cardiac catheterization, and retinal vascular caliber was measured from these photographs by using a computer program and summarized as central retinal arteriolar (CRAE) and venular (CRVE) equivalents. Results: Retinal arteriolar and venular calibers were not associated with increasing severity of CAD, as assessed by Leaman scores (CRAE/CRVE: P for trend=0.17/0.57), presence of clinically significant CAD (CRAE/CRVE: P=0.35/0.32), or number of diseased vessels (CRAE/CRVE: P for trend=0.18/0.69). Conclusions: Retinal vascular caliber changes are not associated with the severity of obstructive CAD in symptomatic patients. These data suggest that the association of retinal vascular caliber with clinical CAD seen in epidemiological studies may not be applicable to clinical symptomatic patients and may be related to microvascular, rather than macrovascular, mechanisms.     

Evaluation of insulin resistance in obese women with and without acanthosis nigricans

Acanthosis nigricans is characterized by hyperpigmented velvety plaques of body folds and neck. Insulin could be a responsible factor in the pathogenesis of this condition and hyperinsulinemia: a consequence of insulin resistance stimulates the formation of these characteristic plaques. In this study, insulin resistance was compared in obese women with and without acanthosis nigricans. This was a cross-sectional study. Sixty-six obese women (32 patients with acanthosis nigricans and 34 patients without acanthosis nigricans) were selected randomly. Levels of fasting serum insulin and fasting blood glucose were measured in both groups and insulin resistance was determined using homeostasis model assessment. Glucose tolerance test also was performed for all of participants. Five (15.6%) patients with acanthosis nigricans and no (0%) patient without acanthosis nigricans had insulin resistance ( P  < 0.05). Six (18.7%) patients with acanthosis nigricans and one (2.9%) patient without acanthosis nigricans had impaired glucose tolerance test ( P  < 0.05). The mean levels of fasting serum insulin were 15.7 ± 8.7 and 12.2 ± 4.1 µm/mL ( P  < 0.05) and the mean values of insulin resistance index were 3.5 ± 1.9 and 2.6 ± 0.9 µm/mL between patients with and without acanthosis nigricans, respectively ( P  < 0.05). In Iranian obese women, acanthosis nigricans is a marker of insulin resistance.     

Urological complications in 980 consecutive patients with renal transplantation

Aim: To present the urological complications of renal transplantations performed in the last 14 years at one center and to briefly explain a modified method of Lich–Gregoir ureteroneocystostomy.
Methods: The data of 980 patients receiving kidney transplants at the authors' institution from April 1991 to February 2004 were reviewed in a retrospective prospective study. In particular, surgical techniques and urological complications were noted.
Results: A total of 980 patients had received kidney transplantation. Extravesical ureteroneocystostomy (Lich–Gregoir method) was used in the first 480 patients (group A). In the subsequent 500 patients, the authors' modified method of extravesical ureteroneocystostomy, using single layer anastomosis and small feeding tubes as stent, was used (group B). Overall urological complication rate was 2.8% (28 patients), including leakage (13 patients, 1.3%), stenosis (seven, 0.7%), obstruction (one, 0.1%), distal ureter necrosis (four, 0.4%), pelvocalyceal fistula (two, 0.2%) and implantation of ureter into the peritoneum (one, 0.1%). Urological complications were significantly more common in group A compared to group B (16, 3.3% and 9, 1.8%, respectively; P  < 0.05).
Conclusions: Preserving the adventitia, fat and blood supply of the ureter by delicate dissection of the ureter during donor nephrectomy, short ureters, and fixation of the adventitia, fat and blood supply of the ureter to the bladder wall, to prevent kinking or twisting, are important factors in decreasing urological complications. Additionally, the authors' method of ureteroneocystostomy is also effective in decreasing the incidence of ureteric complications.     

Is it Safe to Close ASD with the Guidance of Transthoraxic Echocardiography in Pediatric Population “Ten Years' Experience of a Single Center”

Objective

Main purpose of this study is to emphasize the usage and safety of transthoracic echocardiography (TTE) in percutaneous atrial septal defect (ASD) closure in appropriate pediatric cases.

Background

Nowadays, percutaneous closure is preferred as treatment modality for ASD in pediatric age group.

Methods

Between the dates December 2003–August 2013; 340 patients whose ASD were closed included in this study. Physical examination, electrocardiogram, TTE were done before the procedure, at the 24th hour, 1st and 6th month after the procedure. After the 6th month, routine control was done annually. Transesophageal echocardiography (TEE) was performed in 184 cases with large, multifenestrated ASD and when TTE views were poor in quality. We selected the 201 patients whose ASD diameter between 10–20 mm and formed 2 homogeneous groups according to the type of echocardiography used (TEE or TTE) in order to compare the role of echocardiography.

Results

The demographic features of patients of 2 groups were similar. There was not any statistically difference between ASD, balloon sizing diameters between the groups. No statistically significant difference in the success, complication, and residual shunt rates was found between the groups. Procedure, fluoroscopy time, and amount were significantly higher in TEE group. When hemodynamic variables except pulmonary blood flow to systemic blood flow (Qp/Qs; right–left atrium mean pressure, pulmonary vascular resistance, and peak‐mean pulmonary arterial pressure) were compared, there was not statistically difference.

Conclusion

TEE is an invasive procedure and requires general anesthesia, therefore, it should not be done routinely in ASD but only in selected cases. If the size and the anatomy of ASD is appropriate, TTE should be preferred primarily in percutaneous ASD closure.

     

Pseudo-tumoral renal actinomycosis

Actinomycosis is a rare granulomatous chronic infection that is localized most frequently in the cranio-cervical region. Renal localization is exceptional. The authors report a new case of pseudo-tumoral actinomycosis and discuss diagnostic and treatment issues of this disease.     

Are laboratory tests necessary in making the diagnosis of limb pains typical for growing pains in children?

BACKGROUND: The present study was conducted to determine if performing laboratory tests are necessary to exclude other possible diagnoses in a child with limb pains typical for growing pains according to history and physical examination. METHODS: A matched case-control study was carried out on children with limb pains who attended the Motahary clinic, Shiraz, Iran, in a 2 year period. The inclusion criteria were limb pains, which were recurrent and lasted for more than 3 months. The exclusion criteria were any abnormal systemic symptoms and signs, localizing signs, joint involvement; and limp or limitation of activity. The controls were clinically normal children matched for age and sex. Laboratory tests including complete blood count, erythrocyte sedimentation rate, serum calcium, phosphorus, alkaline phosphatase and rheumatoid factor were done for all patients and controls. RESULTS: In total, 100 patients and 150 controls were included in the study. There were no significant differences between the patients and controls with regard to all of the measured laboratory tests. CONCLUSION: Growing pain is a clinical diagnosis and if precise inclusion and exclusion criteria in history and physical examination are considered, there will be no need for laboratory tests in order to make a diagnosis.     

Electrophysiologic Characteristics of Accessory Atrioventricular Connections in an Inherited Form of Wolff-Parkinson-White Syndrome

INTRODUCTION: A familial form of Wolff-Parkinson-White syndrome (WPW) occurs in association with hypertrophic cardiomyopathy and intraventricular conduction abnormalities. This syndrome, demonstrating autosomal dominant inheritance and segregating with a high degree of penetrance but variable expressivity, has been genetically linked to chromosome 7q3. The purpose of this study is to detail the electrophysiologic characteristics of accessory atrioventricular connections (AC) in four members of a kindred with this syndrome. METHODS AND RESULTS: We clinically evaluated 32 members of a single kindred and identified 20 individuals with ventricular preexcitation, abnormal intraventricular conduction including complete AV block and/or ventricular hypertrophy. Genetic linkage analysis mapped the disease gene in this kindred to the chromosome 7q3 locus (maximum logarithm of the odds score = 6.88, theta = 0); recombination events in affected individuals reduced the genetic interval from 7 centimorgans (cM) to 5 cM. Electrophysiologic study of four individuals with preexcitation, identified seven AC (1 right sided, 3 septal, and 3 left sided). All four individuals had inducible orthodromic tachycardia; while three had multiple AC. Bidirectional conduction was demonstrated in 6 of 7 AC. Successful ablation was accomplished in 5 of 7 AC. CONCLUSION: The electrophysiologic characteristics and location of AC in family members having this complex cardiac phenotype are similar to those seen in individuals with isolated WPW. Identification of WPW in more than one family member should prompt clinical evaluation of relatives for additional findings of ventricular hypertrophy or conduction abnormalities.     

Penile Kaposi''s sarcomas in a circumcised and HIV-seronegative patient

Kaposi's sarcoma (KS) limited to penis is rare and usually observed in AIDS patients. However, in circumcised and HIV-seronegative patients, KS confined to the penis is extremely rare. We present the case of an HIV-seronegative and circumcised 55-year-old man, who presented with two reddish papules, one 5 mm in diameter on the coronal sulcus near the frenulum, and the other 2 mm in diameter on the glans penis, which were reported as a Kaposi's sarcoma after excision of the lesion.