Access to a Library of 1,3-disubstituted-1,2,3-triazenes and Evaluation of their Antimicrobial Properties.

BACKGROUND: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. OBJECTIVE: The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential. METHODS: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433. RESULTS: All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginosa and 0.64 µM against Enterococcus faecalis and Pseudomonas aeruginosa. CONCLUSION: Comparing the structure activity relationship, electron withdrawing groups appear to increase antimicrobial activity.

[Zenker´s diverticulum in a hemodialysis patient]. / Diverticule de Zenker chez une patiente en hémodialyse.

Zenker's diverticulum is a rare and generally benign condition. Its occurrence in a hemodialysis patient has therapeutic and prognostic implications and is a risk factor for mortality and morbidity due to its complications, such as protein-energy malnutrition and pneumonitis. We here report a case of Zenker's diverticulum diagnosed in a chronic haemodialysis patient. The study involved a 61-year-old female patient admitted with upper gastrointestinal bleeding associated with dysphagia. Physical examination showed alteration of general condition and the patient reported an average weight loss of 5 kg in 3 months. Esophagogastroduodenal transit was characterized by dilatation of the cervical esophagus, appearing as a large heterogeneous niche whose upper pole was at the level of the pharyngoesophageal junction. The diagnosis of Zenker's diverticulum was retained. Diverticulectomy by cervical incision was performed. The patient died due to inhalational lung disease in the early postoperative period. Zenker diverticulum is a rare, generally benign disease, but in patients undergoing chronic haemodialysis, it increases mortality and morbidity.

PHYTOCHEMICAL SCREENING, ANTIMICROBIAL AND CYTOTOXICITY STUDIES OF ETHANOL LEAF EXTRACT OF APHANIASENEGALENSIS (SAPINDACEAE).

BACKGROUND: Aphania senegalensis (Sapindaceae) is commonly used in Senegalese traditional medicine to treat pain, inflammation, asthenia, bacterial and fungal infections. The aim of this study was to determine the type of phytochemical constituents present in the ethanol leaf extract and its antimicrobial activity against selected bacterial and fungal pathogens. MATERIALS AND METHODS: The ethanol leaf extract of A. senegalensis was evaluated for its cytotoxic effect in the MTT assay against Vero cells. Flavonoids and tannins were the main constituents of the ethanol leaf extract. RESULTS: The extract inhibited the growth of the three fungal strains used in this study moderately with the lowest MIC obtained for Candidaalbicans (0.16 mg/mL). The extract also inhibited the growth of Aspergillus fumigatus and Cryptococcus neoformans with an MIC of 0.62 mg/mL. For bacterial pathogens, strong inhibition was obtained against Enterococcusfaecalis (ATTC 29212) (MIC 0.08 mg/mL), while moderate inhibition was obtained for Escherichia coli (ATTC 25922) (MIC 0.16 mg/mL) and Staphylococcus aureus (ATTC 29213) (MIC 0.31mg/mL). The extract however did not inhibit the growth of Pseudomonasaeruginosa (ATTC 27853) at the highest concentration (2.5 mg/ml) tested. The ethanol leaf extract of A. senegalensis had a higher cytotoxicity than berberine used as the positive control (LC502.67±0.04 µg/mL and 9.99±0.54 µg/mL respectively). The best selectivity index values was obtained for Enterococcus faecalis (SI = 1.24), followed by Escherichia coli (SI = 0.62) for bacterial pathogens and C. albicans (SI = 0.62) for fungal pathogens. CONCLUSION: The findings of this study suggest that the extracts may not be safe for use in animals infected by some pathogens.

(1S,2S,5S)-2-Methyl-3-oxo-5-(prop-1-en-2-yl)cyclo-hexane-1-carbo-nitrile.

The mol-ecule of the title compound, C11H15NO, contains a cyclo-hexa-none ring, three defined stereocenters and an exocyclic double bond. The crystal structure is the result of a study on the Michael addition reaction of (S)-carvone with sodium cyanide using ionic liquids as the reaction medium and so the absolute configuration is known from the chemistry. The six-membered ring is in a chair conformation.