ABSTRACT
The microbicidal effectiveness against Gram-positive and Gram-negative bacteria and Candida albicans of electrochemical silver ions in aqueous solutions containing nonionic surfactants was investigated. From the perspective of the possible use of anodic silver as a preservative in cosmetic or pharmaceutical preparations, microbicidal efficacy was also studied in oil/water model dispersions. Surfactants and botanical extracts partially inhibited the microbicidal effectiveness of anodic silver. Nevertheless in all the experimental conditions, silver ions reduced the microbial concentration up to 4 log units of the starting inoculum in less than 6 h. The wide microbicidal spectrum and the high rate of kill of silver ions appear, therefore, attractive enough to suggest a possible utilization of anodic silver as a preserving agent.
Subject(s)
Candida albicans/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Silver/pharmacology , Surface-Active Agents/pharmacology , Cosmetics/standards , Electrochemistry , Hydrogen-Ion Concentration , Oils/chemistry , Plant Extracts/metabolism , Regression Analysis , Silver/adverse effects , Silver/chemistry , Solutions , Surface-Active Agents/metabolism , Water/chemistryABSTRACT
Owing to the increasing need of drugs for the treatment of a variety of fungal and bacterial opportunistic infections, a study has been started with the aim of synthesizing structures amenable to a number of easily-to-perform structural modifications in order to meet the requirement of bypassing resistance phenomena. This paper reports on the synthesis of several N-(alpha-azaheteroaryl)-substituted 2,5-dimethyl-pyrroles bearing in one beta-position (or in both beta-positions) aminomethyl groups, introduced via a Mannich reaction. Electronic and steric effects by the N-(azaheteroaryl) substituents and the 2- and 5-methyl groups on the course of the Mannich reaction are discussed along with the results of in vitro tests against many Candida species, some bacteria, and several pathogenic plant fungi.
Subject(s)
Anti-Infective Agents/chemical synthesis , Bacteria/drug effects , Fungi/drug effects , Pyridines/chemical synthesis , Pyrimidines/chemical synthesis , Pyrroles/chemical synthesis , Thiazoles/chemical synthesis , Anti-Bacterial Agents , Anti-Infective Agents/pharmacology , Candida/drug effects , Chemical Phenomena , Chemistry, Physical , Mannich Bases/chemical synthesis , Mannich Bases/pharmacology , Pyridines/pharmacology , Pyrimidines/pharmacology , Pyrroles/pharmacology , Thiazoles/pharmacologyABSTRACT
Various aryl-(1H-imidazol-1-yl)-(isoquinolin-1-yl)methane derivatives have been synthesized and tested as antifungal agents. The new imidazoles have been obtained by the action of 1,1'-sulfinyldiimidazole on aryl-(isoquinolin-1-yl)carbinols, which have been prepared by standard procedures starting from isoquinoline. Among 44 test derivatives only a few have exhibited some antifungal activity, the most active compound (4e) being twofold less potent than miconazole, ketoconazole and bifonazole, used as standard drugs.
