Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer.

A novel naphthylmethylimidazole derivative 1 and its related compounds were identified as 17,20-lyase inhibitors. Based on the structure-activity relationship around the naphthalene scaffold and the results of a docking study of 1a in the homology model of 17,20-lyase, the 6,7-dihydro-5H-pyrrolo[1,2-c]imidazole derivative (+)-3c was synthesized and identified as a potent and highly selective 17,20-lyase inhibitor. Biological evaluation of (+)-3c at a dose of 1mg/kg in a male monkey model revealed marked reductions in both serum testosterone and dehydroepiandrosterone concentrations.

Initial airway management skills of senior residents: simulation training compared with traditional training.

Background: Scenario-based training (SBT) with a computerized patient simulator (CPS) is effective in teaching physicians to manage high-risk, low-frequency events that are typical of critical care medicine. This study compares the initial airway management skills of a group of senior internal medicine residents trained using SBT with CPS during their first year of postgraduate training (PGY) with a group of senior internal medicine residents trained using the traditional experiential method.

Methods: This was a prospective, controlled trial that compared two groups of PGY3 internal medicine residents at an urban teaching hospital.

[Clinical study of adenoid cystic carcinoma of the parotid gland].

We report results of a retrospective study of 12 cases of adenoid cystic carcinoma (ACC) in the parotid gland. Local pain was often observed in ACC among other malignant parotid tumors. Although fine-needle aspiration cytology (FNA) was not effective for preoperative diagnosis, frozen section diagnosis (FS) during surgery showed excellent results.

Achieving housestaff competence in emergency airway management using scenario based simulation training: comparison of attending vs housestaff trainers.

Study Objectives: To evaluate a teaching protocol comparing a critical care attending to a housestaff team in training medical interns in initial airway management skills using a computer-controlled patient simulator (CPS) and scenario-based simulation training (SST).

Design: Prospective, randomized, controlled, unblinded trial.

Setting: Internal medicine residency training program in an urban teaching hospital.

Viability and plasma vitamin K levels in the common bile duct-ligated rats.

The common bile duct-ligated (CBDL) rat, which is widely used as a model of human cirrhosis, rapidly develops secondary biliary cirrhosis (SBC) within 4 weeks. The CBDL rat shows poor viability, however, a detailed examination of the causes of its death has not been made. In this study, we investigated the outcome of bile duct ligation in detail and attempted to extend the life span of this model by feeding the animals a diet supplemented with nutrients.

Secondary shunt procedure for alaryngeal patients in an outpatient clinic.

The shunt procedure used for laryngectomized patients undergoing secondary tracheo-esophageal (T-E) puncture is inconvenient and causes stress to the patient. In order to overcome these problems we developed a novel surgical T-E shunt technique using the Groningen voice prosthesis that does not require esophagoscopy or general anesthesia and can be performed in an outpatient clinic. In this procedure, a shunt is created using a pair of nasal forceps with the patient seated.