In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives.

Under three different reaction conditions (conventional heating, microwave irradiations and amino acid catalysis), a series of imidazolylpyrazoles (2a-2k) were synthesized in good to excellent yields from a mixture of three precursors: aryl(hetaryl)pyrazole-4-carbaldehydes (1a-1k), benzil and ammonium acetate. α-Glucosidase inhibition assay revealed a new class of highly potent agents wherein each compound displayed significant inhibitory potentials (in terms of percentage inhibition and relative IC50 values) as compared to that of the reference drug (Acarbose). Moreover, molecular modelling of most potent compounds 2h, 2j and 2k also helped in understanding the structure and activity relationship.

Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.

A series of tetraarylimidazoles (5A-5O) were prepared by one pot four component condensation reactions of 2-arylindole-3-carbaldehydes, substituted anilines, benzil and ammonium acetate in acetic acid. The synthesized compounds exhibited potent antiurease activity with IC50 values ranging from 0.12 ± 0.06 µM to 29.12 ± 0.18 µM as compared with thiourea. However, low inhibition profiles were observed for lipoxygenase. The data show that tetraarylimidazoles containing a substituted 2-penylindole have emerged as a new class of potent inhibitors of urease enzyme.

Predictors of radial artery size in patients undergoing cardiac catheterization: insights from the Good Radial Artery Size Prediction (GRASP) study.

BACKGROUND: Radial artery occlusion occurs after transradial cardiac catheterization or percutaneous coronary intervention. Although use of a sheath larger than the artery is a risk factor for radial artery occlusion, radial artery size is not routinely measured. We aimed to identify bedside predictors of radial artery diameter. METHODS: Using ultrasound, we prospectively measured radial, ulnar, and brachial artery diameters of 130 patients who presented for elective percutaneous coronary intervention or diagnostic angiography. Using prespecified candidate variables we used multivariable linear regression to identify predictors of radial artery diameter. RESULTS: Mean internal diameters of the right radial, ulnar, and brachial arteries were 2.44 ± 0.60, 2.14 ± 0.53, and 4.50 ± 0.88 mm, respectively. Results for the left arm were similar. The right radial artery was larger in men than in women (2.59 vs 1.91 mm; P < 0.001) and smaller in patients of South Asian descent (2.00 vs 2.52 mm; P < 0.001). Radial artery diameter correlated with wrist circumference (r(2) = 0.26; P < 0.001) and shoe size (r(2) = 0.25; P < 0.001) and weakly correlated with height (r(2) = 0.14; P < 0.001), weight (r(2) = 0.18; P < 0.001), body mass index (r(2) = 0.07; P = 0.002), and body surface area (r(2) = 0.22; P < 0.001). The independent predictors of a larger radial artery were wrist circumference (r(2) = 0.26; P < 0.001), male sex (r(2) = 0.06; P < 0.001), and non-South Asian ancestry (r(2) = 0.05; P = 0.006; final model r(2) = 0.37; P < 0.001). A risk score using these variables predicted radial artery diameter (c-statistic, 0.71). CONCLUSIONS: Wrist circumference, male sex, and non-South Asian ancestry are independent predictors of increased radial artery diameter. A risk score using these variables can identify patients with small radial arteries.

Long-term outcomes using a two-stent technique for the treatment of coronary bifurcations.

BACKGROUND: The crush and culotte are probably the most common two-stent techniques utilized for percutaneous coronary intervention (PCI) of complex bifurcation lesions. Long-term outcome associated with the utilization of these techniques is unknown. Our objective was to evaluate the long-term outcomes after bifurcation PCI utilizing these 2 techniques with a prospective PCI registry. METHODS: Between 11/1/2003 and 12/31/2007, 360 patients were treated with either crush (n=304) or culotte (n=56). Primary outcome was the occurrence of major adverse cardiac events (MACE) defined as the composite of death, myocardial infarction and target vessel revascularization. The major secondary outcome measure was MACE or occurrence of CCS Class ≥ 2 angina. RESULTS: After a median follow-up of 4.1 years (3.0-5.1), the occurrence of MACE was 23.9%. MACE or CCS Class ≥ 2 angina occurred in 27.5% of patients. Multivariable analysis revealed that creatinine clearance <60 ml/min (odds-ratio [OR]=1.71, 95% CI 1.08-2.71; p=0.022) and left ventricular ejection fraction <40% (OR=2.14, 95% CI 1.21-3.79; p=0.008) were independent predictors of MACE or CCS Class ≥ 2 angina. A larger main vessel reference diameter (OR=0.57, 95% CI 0.61-0.92), bifurcation angle <50% (OR=0.59, 95% CI 0.35-0.92) and a final kissing-balloon inflation (OR=0.75, 95% CI 0.35-0.99) were associated with a lower risk of MACE or CCS Class ≥ 2 angina. CONCLUSIONS: Application of the crush and culotte techniques is associated with efficacy and safety at long-term follow-up. Bifurcation angle, a final kissing balloon inflation and vessel reference diameter are important variables that impact on very long-term outcomes.

(4Z)-4-[(2E)-1-Hy-droxy-3-(3-nitro-phen-yl)prop-2-en-1-yl-idene]-3-methyl-1-(4-methyl-phen-yl)-1H-pyrazol-5(4H)-one.

In the title compound, C(20)H(17)N(3)O(4), the dihedral angles between the heterocyclic ring and the toluene and nitro-benzene rings are 4.21 (15) and 11.43 (14)°, respectively. The whole mol-ecule is close to planar (r.m.s. deviation for the 27 non-H atoms = 0.171 Å). Two S(6) rings are formed due to intra-molecular C-H⋯O and O-H⋯O hydrogen bonds. In the crystal, inversion dimers linked by pairs of C-H⋯O bonds generate R(2) (2)(10) loops and further C-H⋯O bonds link the dimers along the b-axis direction. There exist π-π inter-actions between the heterocyclic rings at a centroid-centroid distance of 3.7126 (10) Šand between the centroids of the benzene rings at a distance of 3.8710 (16) Å.