Self-Assembled Silica Nanostructures: Simultaneous Discrimination of Handedness, Pitch and Diameter of Helical Silica Nanotubes.

The left- and right-handed helical silica nanostructures were obtained with the aid of organic templates, the formation of the nanostructures might follow a co-operation self-assembly mechanism. The chirality of the organogel self-assemblies was successfully transcribed in to the silica. The helical pitch and pore size of the silica nanotubes sensitively depended on the optical purity of the neutral gelator in the reaction mixtures.

Efficacy and safety of the simultaneous administration of mirodenafil and an α-blocker in men with BPH-LUTS: a multicenter open-label prospective study.

We evaluated the clinical efficacy and safety of the coadministration of a PDE5 inhibitor and an α-adrenergic blocker in patients with both benign prostatic hyperplasia/lower urinary tract symptoms (BPH-LUTS) and ED using mirodenafil 50 mg (Mvixx) once daily (OD) in patients already receiving stable α-blocker therapy. This study was a prospective, multicenter, open-label trial. We selected 147 patients undergoing stable (longer than 4 weeks) α-blocker therapy for BPH-LUTS as recipients of the additive mirodenafil 50 mg OD for 8 weeks. The coprimary measures were the International Prostate Symptom Score (IPSS) and the International Index of Erectile Function (IIEF-5). The key secondary measures were peak flow rate (Qmax) and postvoiding residual (PVR) volume. Safety was assessed by evaluating cardiovascular parameters and the participant-reported treatment-emergent adverse events (TEAEs). The additional administration of mirodenafil 50 mg OD significantly improved IPSS results (18.70-14.30 at 4 weeks and 18.70-13.72 at 8 weeks; P<0.001). The IIEF-5 score was improved at 8 weeks (10.94-16.16; P<0.001). There was no significant change in systolic blood pressure/diastolic blood pressure (124.8 mm Hg/78.6 mm Hg-122.0 mm Hg/79.6 mm Hg; P=0.638) and heart rates (78.8 per min to 80.2 per min; P=0.452). The most common TEAEs were hot flashes (10.9%) and headache (8.1%). The combination of mirodenafil with an α-blocker did not significantly improve PVR; however, Qmax was improved at 8 weeks (14.51-16.80 ml s(-1); P=0.026). Mirodenafil 50 mg OD in combination with an α-blocker appeared to have few adverse effects, to improve BPH-LUTS and restore sexual function.

Efficacy and safety of combination therapy with mirodenafil and α1-blocker for benign prostatic hyperplasia-induced lower urinary tract symptoms accompanied by erectile dysfunction: a multicenter, open-label, prospective study.

This study was conducted to determine whether mirodenafil 100 mg, when administered on demand to patients with benign prostatic hyperplasia (BPH) who are receiving α1-blocker therapy, is safe with regard to the cardiovascular system and whether it improves lower urinary tract symptoms (LUTS) and sexual function. The study involved 121 LUTS/BPH patients who had been treated for at least 3 months with α1-blockers before being administered with mirodenafil 100 mg on demand. Before the start of mirodenafil administration, the blood pressure, heart rate, international prostate symptom score (IPSS)/quality of life (QoL), peak urine flow rate (Qmax), post-voiding residual urine volume (PVR), and international index of erectile function-5 (IIEF-5) of each patient were measured. At 4 and 8 weeks after commencing mirodenafil administration, the blood pressure and heart rate were measured again, any adverse effects of mirodenafil were assessed, and sexual function and voiding symptoms were re-evaluated. Of the 121 patients, 73 (60.3%) completed the 8-week clinical trial. Significant changes in blood pressure and heart rate were not observed during the study. Significant improvements in the IIEF-5 and the IPSS/QoL, but not the Qmax or PVR, were observed. The results of this study suggest that the administration of mirodenafil 100 mg on demand may induce few hypotensive interactions and may be acceptably effective with regard to improving LUTS and sexual function.

Safety and efficacy of the simultaneous administration of udenafil and an alpha-blocker in men with erectile dysfunction concomitant with BPH/LUTS.

We evaluated the clinical efficacy and safety of administering udenafil (5-[2-propyloxy-5-(1-methyl-2-pyrollidinylethylamidosulphonyl)phenyl]-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)-pyrimidin-7-one) in patients with comorbid benign prostatic hyperplasia (BPH) and erectile dysfunction (ED). One hundred and twenty patients who had been undergoing stable alpha-blocker therapy for BPH were enrolled in this trial and they were administered 100 mg udenafil for 8 weeks. Changes in blood pressure (BP), heart rate (HR), the international prostatic symptom score (IPSS) and the international index of ED (IIEF-5) were evaluated every 4 weeks. At end point, there was no significant change in BP and HR, whereas the lower urinary tract symptoms (LUTS) and ED improved significantly compared with baseline (IPSS 14.3-11.5, IIEF-5 11.95-18.32, P<0.05). Most patients were tolerant to the treatment and there was no evidence of additional side effects related to coadministration. The coadministration of udenafil and an alpha-blocker in patients with comorbid BPH and ED was safe and gave significant improvements in both LUTS and ED.

Sexuality and the management of BPH with alfuzosin (SAMBA) trial.

The sexuality and the management of benign prostatic hyperplasia (BPH) with alfuzosin (SAMBA) trial evaluated the effect of alfuzosin on sexual function in men treated for BPH using two sexual function scales: male sexual health questionnaire (MSHQ) and international index of erectile function (IIEF-15). A total of 148 patients with BPH were treated with alfuzosin for 24 weeks. The patients were followed at baseline, 4, 12 and 24 weeks after medication with alfuzosin. MSHQ was collected at every visit, whereas Q(max), IPSS and IIEF-15 were checked at baseline and end point. At the end point, Q(max) (+4.7 ml s(-1), P<0.01) and IPSS (-5.3, P<0.01) had improved significantly. Alfuzosin also significantly improved the total MSHQ (19.2%, 79.1-94.3, P<0.01) and the MSHQ ejaculatory scores (26.0%, 22.3-28.1, P=<0.01) versus baseline. Alfuzosin for the treatment of patients with BPH is effective in improving sexual function, as well as lower urinary tract symptoms (LUTSs) and quality of life, and is well tolerated.

Facile and efficient total synthesis of (+)-preussin.

[structure] The enantioselective total synthesis of (+)-preussin, a potent antifungal agent, has been achieved. The key steps are a Pd(0)-catalyzed oxazoline-forming reaction from L-phenylalanine, hydrogenolysis, and subsequent diastereoselective reductive cyclization of the intermediate aminoketone to pyrrolidine using Pearlman's catalyst.

Synthesis and characterization of stereospecific 1-propargyl-2-(dimethoxymethyl)-1-cyclohexanols.

Stereochemical isomers with hydroxy groups were synthesized by reacting 2-(dimethoxymethyl)cyclohexanone with propargylmagnesium bromide. The stereo chemical structures were identified by NMR spectral interpretation and the geometry optimization. To assist the NMR interpretation, geometry optimization based on semi-empirical AM1 and PM3 methods was applied. Throughout this study, the structures of the two isomers were all determined and 1H and 13C NMR spectra were fully assigned. It was proven that the less polar isomer is an axial alcohol and the more polar one is an equatorial alcohol.

Total synthesis of (+/-)-homoepibatidine.

Total synthesis of (+/-)-homoepibatidine (2), which contains the 8-azabicyclo[3.2.1] octane ring system, was achieved by using palladium-catalyzed Heck-type coupling reaction from 3.

Stereoselective synthesis of (+/-)-epibatidine analog:(+/-)-2beta-(2-chloro-5-pyridinyl)-8-azabicyclo[3.2.1] octane.

Stereoselective synthesis of (+/-)-epibatidine analog 2, which contains the 8-azabicyclo[3.2.1]octane ring system, was achieved by using palladium-catalyzed Heck-type coupling reaction from 3.