Based on preliminary molecular modelling study, the synthesis of two different classes of biphenylyltetrazole derivatives of 1-aminopyrroles, as potentially active non-peptide angiotensin II (AII) antagonists, is reported. Some NH-Boc protected l-aminopyrroles were deprotected, N-acylated, N-alkylated with 5-[4'-bromomethyl-1,1'-biphenyl-2-yl]-1-triphenylmethyl-1H-tetrazo le, and then detritylated to give the first class of title compounds. Other 1-NH-Boc protected 1,2-diaminopyrroles were regioselectively subjected to the 1-alkylation with 5-[4'-bromomethyl-1,1'-biphenyl-2-yl]-1-triphenylmethyl-1H-tetrazo le, to the acylation of the amino group at 2-position of the pyrrole ring, and then to the detritylation process to yield the second class of title compounds.

Adrenal Cortex↗

PubMedDate not supplied

Researches on psychotropic agents. IV. Synthesis and neuropsychopharmacological effects of 1,3,4,14 b-tetrahydro-10-methyl-2H,10H- pyrazino[2,1-d] pyrrolo[1,2-b][1,2,5]benzotriazepine and its derivatives.

The synthesis and neuropsychopharmacological properties of new 1,3,4,14b-tetrahydro-2H,10H-pyrazino [2,1-d] pyrrolo [1,2-b] [1,2,5] benzotriazepine derivatives related to antidepressant agent aptazepine are reported. The new derivatives displayed sedative-miorelaxant activity in mice, but no significant antagonist effect on clonidine blockade of phenylquinone-induced abdominal constriction. Among test compounds 4a, 4l and 4n showed high antinociceptive effect on the hot-plate test and compound 4e protected from death and convulsion all the electroshocked animals.

Analgesics↗

PubMedDate not supplied

High negative predictive value of slow lymphatic drainage on metastatic node spread detection in malignant limb and trunk cutaneous melanoma.

AIM: Harvesting of the "sentinel lymph node" (SLN) as identified by lymphoscintigraphy (LSG) is becoming increasingly important in the staging of patients with malignant melanoma. The purpose of the current study was to determine whether the appearance time of the LSG had a prognostic value in predicting metastasis dissemination in thick cutaneous malignant melanoma. METHODS: Between July 1999 and July 2003, 88 consecutive patients with histologically proven melanoma with a Breslow's thickness > 1 mm, without clinical or radiological evidence of lymph node involvement or metastasis, prospectively underwent lymphoscintigraphy with 32 Mbq Tc 99m sulfur colloid prior to sentinel lymphadenectomy with sentinel lymph node (SLN) histological examination. RESULTS: LSG was performed in 88 patients with limb and trunk melanoma and identified a total of 149 sentinel nodes. Pathological examination revealed lymph node involvement in 21 patients (24%). All positive SLNs were imaged with a scintigraphic appearance time of less than 30 min. With a scintigraphic appearance time greater than 30 min, the negative predictive value (NPV) of spread in the SLN was 100% (27/27)(CI 87-100%). CONCLUSION: The strong NPV of LSG in identifying "slow" sentinel lymph nodes in patients with no clinical evidence of lymph node involvement suggests that patients could be spared sentinel lymph node biopsy when LSG detects "slow" sentinel lymph nodes. Another prospective study will be required to confirm that the scintigraphic appearance time of sentinel lymph nodes is an important predictive parameter of metastatic disease in sentinel lymph nodes and consequently might reduce the number of sentinel lymph node biopsies.

Adult↗

PubMedDate not supplied

[Acute secondary and transitory erythroblastopenia in kwashiorkor under treatment].

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Anemia↗

PubMedDate not supplied

[Intravenous immunoglobulins in bone marrow transplantation].

Intravenous immunoglobulins have a role also in the prevention of infections after a bone marrow transplantation. Even if a reduction of CMV pneumonia is reported it is not clear whether such an effect is due to a direct antiviral activity or it is mediated through an immune modulation that reduces GVHD and then the immune suppression. We are currently using i.v.Ig at a dose of 100 mg/kg/day within a protocol for GVHD prophylaxis after a mismatched BMT.

Bone Marrow Transplantation↗