ABSTRACT
Chondrosarcoma is a tumor very seldom encountered in the larynx. In this location chondrosarcomas have typical features: slow growing, metastasis rares and scarce tendency to recur. But recurrences occurs at long-term and often can be controlled. We report a case diagnosed and treated in our Hospital which, on the contrary, recurrences presented in a short-term after first surgical removal. Clinical management and treatment of these neoplasms are reviewed.
Subject(s)
Chondrosarcoma/diagnostic imaging , Chondrosarcoma/pathology , Laryngeal Neoplasms/diagnostic imaging , Laryngeal Neoplasms/pathology , Adult , Chondrosarcoma/surgery , Humans , Laryngeal Neoplasms/surgery , Male , Neoplasm Staging , Tomography, X-Ray ComputedABSTRACT
Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field.
Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Ketones/chemical synthesis , Ketones/pharmacology , Methanol/analogs & derivatives , Nitroimidazoles/chemical synthesis , Nitroimidazoles/pharmacology , Microbial Sensitivity Tests , Mutagenicity Tests , Structure-Activity RelationshipABSTRACT
Four series of compounds whose substructure contains a formamidine functionalized as a novel group in the chemistry of histamine H2-receptors have been synthesized. Series design, synthesis and pharmacological data including inhibition of histamine-stimulated acid secretion, inhibition of acid secretion p.o. and pA2 are reported. N-[(E)-[[2-[[[2](Diaminomethylene)amino]-4-thiazolyl] methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide (ebrotidine, CAS 100981-43-9, FI-3542) was selected for further research.
Subject(s)
Amidines/chemical synthesis , Histamine H2 Antagonists/chemical synthesis , Amidines/pharmacology , Animals , Depression, Chemical , Female , Gastric Acid/metabolism , Guinea Pigs , Heart Atria/drug effects , Heart Rate/drug effects , Histamine H2 Antagonists/pharmacology , In Vitro Techniques , Male , Rats , Rats, Sprague-Dawley , Structure-Activity RelationshipABSTRACT
Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl] thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist with a potent antisecretory activity and evidenced gastroprotection. This paper describes its physicochemical properties, spectroscopy for its structural identification, detection methods for its organic and inorganic impurities, purity quantitation and stressed degradation and stability tests in solid and solution forms in order to know the behaviour of the test substance against certain experimental conditions. The results obtained indicate that ebrotidine is stable for over 3 years normal storage conditions (25 degrees C/75% RH). As ebrotidine was not found to be hygroscopic or particularly photosensitive, no special storage precautions are required.
Subject(s)
Benzenesulfonates/chemistry , Histamine H2 Antagonists/chemistry , Thiazoles/chemistry , Chromatography, High Pressure Liquid , Magnetic Resonance Spectroscopy , Mass Spectrometry , Potentiometry , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , X-Ray DiffractionABSTRACT
Compound 1 (1-benzyl-3-methyl-4-[4-(4-fluorophenyl)-4-oxobutyl]piperazine), a synthetic intermediate identified as a potential atypical antipsychotic, was selected as the starting point for pharmacological improvement. From 1, sequential structural variations were conducted in order to improve its potency and oral bioavailability. These variations included a series of piperazine, ethanediamine, and piperidine derivatives. The piperidine series afforded some orally potent compounds in the inhibition of apomorphine-induced climbing and hyperactivity in mice, which are regarded as behavioral models predictive of antipsychotic efficacy. Further optimization of these structures led to the highly potent 7-[3-(1-piperidinyl)propoxy]chromenones. Inhibition of stereotypies and induction of catalepsy in rats at doses substantially higher than required for inhibition of climbing suggest an atypical antipsychotic profile, which is assumed to predict a reduced induction of extrapyramidal side effects in humans.
Subject(s)
Antipsychotic Agents/chemical synthesis , Chromones/chemical synthesis , Administration, Oral , Animals , Antipsychotic Agents/pharmacokinetics , Antipsychotic Agents/pharmacology , Apomorphine/pharmacology , Behavior, Animal/drug effects , Biological Availability , Catalepsy/chemically induced , Chromones/pharmacokinetics , Chromones/pharmacology , Male , Mice , Molecular Structure , Motor Activity/drug effects , Rats , Rats, Sprague-Dawley , Stereotyped Behavior/drug effects , Structure-Activity RelationshipABSTRACT
A new series of (benzo[b]thienyl)methyl ethers of 1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethanol and of (Z)-1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethanone oxime were synthesis and tested for antifungal activity. Series design, synthesis, preliminary antimycotic data and structure-activity relationships are reported. 7-Chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1- yl)ethoxymethyl]benzo[b] (8i, Sertaconazole, FI-7045, CAS 99592-32-2) and its nitrate were selected for further research.
