Simple Synthetic Approach to N-(Pyridin-2-yl)imidates from Nitrostyrenes and 2-Aminopyridines via the N-(Pyridin-2-yl)iminonitriles as Intermediates.

A facile, green, synthetic protocol of several substituted N-(pyridin-2-yl)imidates from nitrostyrenes and 2-aminopyridines via the corresponding N-(pyridin-2-yl)iminonitriles as intermediates is reported. The reaction process involved the in situ formation of the corresponding α-iminontriles under heterogeneous Lewis acid catalysis in the presence of Al2O3. Subsequently, α-iminonitriles were selectively transformed into the desired N-(pyridin-2-yl)imidates under ambient conditions and in the presence of Cs2CO3 in alcoholic media. Under these conditions, 1,2- and 1,3-propanediols also led to the corresponding mono-substituted imidates at room temperature. The present synthetic protocol was also developed on one mmol scale, providing access to this important scaffold. A preliminary synthetic application of the present N-(pyridin-2-yl)imidates was carried out for their facile conversion into the N-heterocycles 2-(4-chlorophenyl)-4,5-dihydro-1H-imidazole and 2-(4-chlorophenyl)-1,4,5,6-tetrahydropyrimidine in the presence of the corresponding ethylenediamine and 1,3-diaminopropane.

Robotic Bronchoscopy in Lung Cancer Diagnosis.

BACKGROUND: The widespread use of chest CT has increased the number of detected pulmonary nodules. Nodules with intermediate risk of malignancy warrant further evaluation with PET-CT or sampling. Although sampling with conventional bronchoscopy presents lower complication rates compared to transthoracic needle biopsy (TTNB), it is limited by the inability to reach distal airways. To overcome this shortcoming, a new bronchoscopic technique named robotic bronchoscopy (RB) has emerged. METHODS: A literature review was used to clarify the rationale behind RB emergence, describe RB procedure, and summarize data regarding its efficacy and safety. RESULTS: The FDA has approved three RB platforms for clinical use. RB is safe, presenting a mortality and complication rate of 0% and 0-8.1%, respectively. Common complications include pneumothorax (0-5.7%) and minor bleeding (0-3.2%). However, its diagnostic yield remains lower than that of TTNB. CONCLUSIONS: RB is a promising bronchoscopic technique that aims to overcome the limitations of conventional bronchoscopy and improve upon the current techniques of guided bronchoscopy for the investigation of pulmonary nodules. Despite the lower complication rate, current evidence suggests a lower diagnostic yield compared to TTNB. Additional studies are required to adequately evaluate the role of RB in the diagnosis of pulmonary nodules.

Targeted therapy for nonsmall cell lung cancer: focusing on angiogenesis, the epidermal growth factor receptor and multikinase inhibitors.

Chemotherapy used to be the only available option to fight advanced nonsmall cell lung cancer. Platinum-based medication combined with taxanes, vinca alkaloids, and antimetabolites improved patient survival rates. Unfortunately, neoplasmatic diseases remain a global killer because chemotherapy benefits have reached a plateau and most patients are diagnosed at the metastatic stage. The urgent need for therapeutic agents, along with advances in the knowledge of the molecular events of oncogenesis, has resulted in the development of medication that specifically targets processes and pathways critical for tumor growth, such as angiogenesis and the epidermal growth factor receptor. Initially, inhibiting these pathways managed to prolong patient survival, although not to the extent desired. Moreover, targeted therapy combined with conventional cytotoxic agents has shown no superiority to chemotherapy alone in terms of patient survival. Hence, numerous multidynamic agents have appeared in the hope that they might help fight nonsmall cell lung cancer. However, no group of patients who will hopefully gain maximum benefit from such interventions has been clearly identified yet. This paper presents current evidence with regard to such novel agents and angiogenesis and epidermal growth factor inhibitors.

Therapy-induced toxicity of the lungs: an overview.

UNLABELLED: Pulmonary toxicity induced by novel antineoplastic agents has not been well characterized because of the simultaneous or sequential use of drugs and a multimodality therapeutic approach. To further investigate this topic, relevant studies were identified through Medline. The generic names of novel antineoplastic agents and the key words pulmonary toxicity, dyspnea and pneumonitis were used for the search. References from the articles identified were also reviewed for additional sources. Most novel antineoplastic drugs may induce pulmonary toxicity. The most recognized patterns of lung toxicity consist of unspecified dyspnea and interstitial lung disease (ILD). Exclusion diagnosis of possible underlying diseases is necessary. Genetic predisposition, autoimmune conditions or superimposed disease may also be involved in the development of lung toxicity. CONCLUSION: Clinicians should be aware of potential pulmonary toxicity as a complication in the treatment of cancer and focus on its early detection or prediction.

Pneumonitis related to docetaxel: case report and review of the literature.

Taxotere has recently been making a noticeable impact on breast, gastric, ovarian, prostate and non-small cell lung cancers. Its side effects include dyspnea, pruritus, skin rashes, fever and hypotension. The patient presented the less common, however potentially fatal, toxicity of pneumonitis. He initially presented with a flu-like illness and hypoxia that was unresponsive to antibiotic treatment and actually progressed. He presented 14 days after his second dose of taxotere, although in retrospect noted symptoms several days prior. Although some patients described in the literature have progressed to respiratory failure requiring mechanical ventilation, this patient responded to steroid treatment and withdrawal of taxotere.

PET/CT and brain MRI role in staging NSCLC: prospective assessment of the accuracy, reliability and cost-effectiveness.

AIM: To determine whether PET/CT and brain MRI used in staging NSCLC can be accurate, reliable and cost-effective tools. NSCLC represents 80-85% of lung cancer and adequate information on the initial tumor staging is critical for planning an optimal therapeutic strategy. PATIENTS & METHODS: Data from 30 newly diagnosed NSCLC patients in Greece were collected and prospectively recorded. Patients with potential resectable disease were evaluated to ensure that there are no detectable metastases that would rule out the possibility of a curative surgery. RESULTS: Divergence occurred in 50% of cases of staging with CT or PET/CT alone, while metastases undetectable by the CT were revealed using PET/CT. Unnecessary thoracotomies were avoided by 10% of patients and another 10% was operated on after chemotherapy with a better prognosis. CONCLUSION: PET/CT and brain MRI combined are reliable for correct staging, reducing avoidable thoracotomies, morbidity rates and costs.

Cervical chordoma in childhood: clinical statistical contribution.

Parapharyngeal neoplasias are rarely noticed in childhood, since they have their peak incidence between the 2nd and 4th decade of life. The authors report a case of a 4-year-old patient presenting with a retrostyloid mass, accompanied by nasal obstruction and some difficulty in swallowing at 12 months of age. CT scanning well ascertained the delimitation of the tumor, but it was of no help in the differential diagnosis. In fact, after surgical excision, the histological examination of the specimen revealed a chordoma. This result was unexpected because of the region concerned and the lack of a CT demonstration of the cervical boney involvement. A cervical vertebral localization of a chordoma is rare in all age groups and it is of particular clinical and statistical interest in infancy.

Multicystic kidney joined to the homolateral testis by an ectopic vas deferens: embryological hypothesis for a new description.

Ectopic location of the vas deferens is a rare congenital anomaly with multiple variations. The frequent association with ano-rectal abnormalities and hypospadias is well known. We report two cases of a newborn and a 3-year-old child with ectopic vas deferens coupled with a left multicystic kidney without any ureteral structure. Furthermore, the latter had a contralateral vesicoureteral reflux and anal agenesis with recto-bulbar fistula. Our attempt with this report is to explain the development of such anomalous deferential outlet into the multicystic kidney, according to the most qualified theory of the Wolffian duct embryology.

Eustachian tube permeability during the nasal provocation test.

The results of manometric study on the permeability of the Eustachian tube after a crisis has been produced by exposing 26 cases of perennial nasal atopy to the threshold-dose of the responsible allergen are reported. In 73% of the cases a reduction of the permeability (16 cases) or a stenosis (4 cases) of the ipsilateral tube were found. The importance of inquiring and specifically treating a nasal allergy in patients suffering from secretory otitis is underlined.

[Thymopentin in the treatment of recurrent condylomata acuminata]. / La timopentina nel trattamento dei condilomi acuminati recidivanti.

Twelve patients who had been suffering from genital and/or perianal recurrent condyloma acuminatum for a minimum of 5 to a maximum of 24 months, in spite of treatment, were studied from the immunological viewpoint and treated with 50 mg s.c. Thymopentin three times a week for 4 or 6 weeks. Six of the patients were cured at the end of treatment, five after 5 months, and one was not cured. Analysis of the clinico-laboratory data shows a significant agreement between the course of clinical signs and the immunological picture. The various cure stages are probably attributable to the basic immune arrangement which was more impaired in the 5 patients who were cured more slowly and in the non-cured case. In the latter too, however, Thymopentin permitted correcting the balance of the relationship between the various lymphocyte subpopulations.

Magnetoliposomes and their potential in the intelligent drug-delivery field.

Research advancements for magnetically guided drug delivery encompass not only the improvement of the design, synthesis and evaluation of more selective nanomaterials bearing magnetic properties, but also the optimization of the transport and delivery of magnetic agents. Such versatile platforms can be utilized for simultaneously carrying therapeutics and diagnostics.

The renal-resistive index from the last 3 months of pregnancy to 6 months old.

OBJECTIVE: To measure the renal resistive index (RI, an estimate of renal vascular resistance, used to assess upper tract obstructive uropathy) from the last trimester of pregnancy to the sixth month of life in a large series of healthy subjects, and thus to identify normal values that can be used routinely. During the first semester of life significant haemodynamic changes during the physiological development of the kidney cause considerable variability in RI, which is thus considered less reliable in this period. SUBJECTS AND METHODS: From September 1998 to October 1999, 93 subjects (186 renal units, RU) were enrolled; 32 were fetuses in the last trimester of pregnancy (group 1, 64 RU) and 61 were children (122 RU), 30 aged 0-1 month (group 2, 60 RU), 20 aged 1-3 months (group 3, 40 RU) and 11 aged 3-6 months (group 4, 22 RU). All subjects underwent colour Doppler ultrasonography and the RI of the renal artery was measured for each kidney. RESULTS: The RI was very high in group 1 but decreased noticeably during the first 6 months of life, reaching values similar to those in adults after the third month. The variability in RI continuously declined with age, becoming less important. The normal ranges for groups 1-4 were 0.67-0.88, 0.57-0.90, 0.60-0.84 and 0.65-0.75, respectively. There were no statistically significant differences between the left and right kidneys. CONCLUSION: In the first semester of life there is more than one landmark value of RI depending on the month of age of the infant. This should be considered when assessing upper tract obstructive uropathies after birth and the RI should be compared with the normal ranges reported herein.