Subject(s)
Echinococcosis, Hepatic/drug therapy , Adolescent , Adult , Aged , Aged, 80 and over , Albendazole/adverse effects , Albendazole/pharmacokinetics , Albendazole/therapeutic use , Anthelmintics/administration & dosage , Anthelmintics/adverse effects , Anthelmintics/pharmacokinetics , Anthelmintics/therapeutic use , Antinematodal Agents/administration & dosage , Antinematodal Agents/adverse effects , Antinematodal Agents/pharmacokinetics , Antinematodal Agents/therapeutic use , Child , Drug Resistance , Ethanol/administration & dosage , Ethanol/therapeutic use , Female , Forecasting , Humans , Injections, Intralesional , Male , Mebendazole/adverse effects , Mebendazole/pharmacokinetics , Mebendazole/therapeutic use , Middle Aged , Paracentesis/methods , Population Surveillance , Recurrence , Time Factors , Ultrasonography, InterventionalSubject(s)
Colonoscopy/adverse effects , Polyethylene Glycols/adverse effects , Respiratory Distress Syndrome/chemically induced , Solvents/adverse effects , Acute Disease , Administration, Inhalation , Aged , Fatal Outcome , Female , Humans , Polyethylene Glycols/administration & dosage , Solvents/administration & dosageABSTRACT
In May 1993, at the end of the rainy season, outbreaks of Paederus sabaeus (Coleoptera, Staphylinidae) were recorded in Brazzaville (Congo), Kinshasa (Zaire), Franceville and Libreville (Gabon) and even in Bangui (CAR) at the North of the equator. A short review of previous outbreaks in Africa and on vesicant substances is given by the authors. These beetles are attracted to neon lights and they rest on the walls or on the skin of the occupants. When the insects are crushed on the bare skin their haemolymph liberate pederine and related vesicant components which provocate dermatitis. The insects disappeared spontaneously after three to four weeks.
Subject(s)
Coleoptera , Dermatitis/epidemiology , Dermatitis/etiology , Animals , Coleoptera/chemistry , Congo/epidemiology , Democratic Republic of the Congo/epidemiology , Gabon/epidemiology , Irritants/poisoning , Pyrans/poisoning , Seasons , Toxins, BiologicalABSTRACT
Potent anticonvulsant activity has been reported for (R,S)-2-acetamido-N-benzyl-2-methylacetamide (2a). Select alpha-heteroatom substituted derivatives of 2a have been prepared (26 examples) in which the alpha-methyl group has been replaced by nitrogen (3a-q), oxygen (3r-u), and sulfur (3v-z) containing moieties. The functionalized amino acid derivatives were evaluated in the maximal electroshock seizure (MES) and horizontal screen (tox) tests in mice. The most active compounds were (R,S)-2-acetamido-N-benzyl-2-(methoxyamino)acetamide (31), and (R,S)-2-acetamido-N-benzyl-2-(methoxymethylamino)acetamide (3n). After ip administration, the MES ED50 values for 31 (6.2 mg/kg) and 3n (6.7 mg/kg) compared favorably with phenytoin (9.50 mg/kg).
Subject(s)
Acetamides/chemistry , Amino Acids/chemistry , Anticonvulsants/chemical synthesis , Acetamides/therapeutic use , Animals , Anticonvulsants/therapeutic use , Chemical Phenomena , Chemistry , Electroshock , Male , Mice , Molecular Structure , Nitrogen , Oxygen , Seizures/etiology , Seizures/prevention & control , Structure-Activity Relationship , SulfurABSTRACT
We recently reported the potent anticonvulsant activity of (R,S)-alpha-acetamido-N-benzyl-alpha-phenylacetamide (2b). Selectively substituted derivatives of this compound have now been prepared (23 examples) and evaluated in the maximal electroshock seizure (MES) and horizontal screen (tox) tests in mice. In several key cases, replacement of the alpha-phenyl substituent in 2b by a relatively small, electron-rich, heteroaromatic moiety led to a substantial improvement in the anticonvulsant potency of the drug candidate. The most active compounds were (R,S)-alpha-acetamido-N-benzyl-2-furanacetamide (2g) and (R,S)-alpha-acetamido-N-benzyl-2-pyrroleacetamide (2i). After ip administration, the MES ED50 values for 2g (10.3 mg/kg) and 2i (16.1 mg/kg) compared well with phenytoin (9.50 mg/kg). Evaluation of the two individual enantiomers of 2g demonstrated that the anticonvulsant activity resided in the R stereoisomer. The low ED50 value (3.3 mg/kg) for (R)-2g contributed to the large protective index (TD50/ED50) observed for this drug candidate, which approached that of phenytoin.
