Adenoid cystic carcinoma with a leptomeningeal dissemination in a ‘wash’ pattern

A 39-year-old woman was referred to the neurology department due to headache, instability and difficulty walking for 5 months. Several ancillary tests were performed. The blood test showed leucocytosis and the cerebrospinal fluid revealed an increased total protein and glucose consumption. Other infections or autoimmune causes were excluded. The MRI showed non-specific brain and spinal cord lesions. Given the findings described, a differential diagnosis between granulomatous meningoencephalitis and primary tumour or metastasis was proposed. Empirical treatment with tuberculostatic agents and corticosteroids was started. The neurological state of the patient worsened, she fell into a non-responsive coma and died in few days. The clinical autopsy performed revealed an adenoid cystic carcinoma with involvement of the central nervous system that developed leptomeningeal dissemination along the spinal cord in a fluid ‘wash’ pattern.

Synthetic approaches to 2-aryl/hetaryl- and 2-(hetaryl)ylidene derivatives of fluorinated 1,3-benzothiazin-4-ones

A series of 2-hetaryl- and 2-(hetaryl)ylidene substituted 5-fluoro-8-nitro-1,3-benzothiazin-4-ones was synthesized by interaction of 2,6-difluoro-3-nitrobenzoylisothiocyanate with C-nucleophiles. Cyclocondensation of polyfluorobenzoylchlorides with aryl and hetaryl thioamides represents new approach to 1,3-benzothiazin-4-ones. Some compounds proved to be promising for further development of tuberculostatic agents.

EVALUATION OF A GROUP OF PYRROLE DERIVATIVES AS TUBERCULOSTATIC AGENTS

: This research aims to contribute to the global search for more effective tuberculostatics that has been triggered by recent outbreaks of tuberculosis. A group of pyrrole-containing derivatives are designed and theoretically elucidated. The identification of the pharmacophore group using the PharmaGist webserver is attempted. Also, the corresponding drug-like properties of the tested compounds are evaluated, together with their possible toxicity risks. The pharmacokinetic behavior of the structures is predicted, based on the Lipinski’s Rule of Five. The effects of some structural parameters are tested. In addition, in vitro evaluations of the anti-tubercular activity against Mycobacterium tuberculosis H37Rv are performed, with compound GA-9 registering the highest activity.

Planarity of benzoylthiocarbazate tuberculostatics. III. Diesters of 3-(2-hydroxybenzoyl)dithiocarbazic acid

Searches for new tuberculostatic agents are important considering the occurrence of drug-resistant strains ofMycobacterium tuberculosis. The structures of three new potentially tuberculostatic compounds, namely isopropyl methyl (2-hydroxybenzoyl)carbonohydrazonodithioate, C12H16N2O2S2, (Z)-benzyl methyl (2-hydroxybenzoyl)carbonohydrazonodithioate, C16H16N2O2S2, and dibenzyl (2-hydroxybenzoyl)carbonohydrazonodithioate propan-2-ol monosolvate, C22H20N2O2S2·C3H8O, were determined by X-ray diffraction. The mutual orientation of the three main fragments of the compounds, namely an aromatic ring, a dithioester group and a hydrazide group, can influence the biological activity of the compounds. In all three of the structures studied, the C(=O)NH group is in theanticonformation. In addition, the presence of the hydroxy group in theorthoposition of the aromatic ring in all three structures leads to the formation of an intramolecular hydrogen bond stabilizing the planarity of the molecules.