The Effect of Some 4,2 and 5,2 Bisthiazole Derivatives on Nitro-Oxidative Stress and Phagocytosis in Acute Experimental Inflammation

Nineteen bisthiazoles were tested in order to assess their anti-inflammatory and antioxidant properties. First, we evaluated the in vitro direct antioxidant capacity of the bisthiazoles using the DPPH radical scavenging method. Then, the anti-inflammatory effect was tested in acute rat experimental inflammation by measuring the acute phase bone marrow response, the phagocytic capacity and the serum nitro-oxidative stress status. Although none of the substances showed significant direct antioxidant potential in the DPPH assay, most of them improved serum oxidative status, when administered to rats with inflammation. Four of the bisthiazoles proved to have good anti-inflammatory properties, similar or superior to that of equal doses meloxicam

SYNTHESIS AND EFFECTS OF SOME NEW 2-ARYL-THIAZOLE AMMONIUM SALTS ON ISOLATED ILEUM MOTILITY

Quaternary ammonium compounds are considered among the substances which can influence the contractility of smooth muscles from the digestive tract, acting via cholinergic mechanisms. Based on structural considerations, we synthesized twelve new compounds, derivatives of 2-aryl-thiazole, being substituted in the 2 and 4 positions. In order to elucidate the structure of the obtained compounds, MS determinations and 1 H-NMR spectra were realized. The effect on the smooth muscles was tested using the guinea pig isolated ileum experimental model. The obtained results showed that the contractile effects or the antispasmodic activity of the compounds are influenced by the nature of the substituent in the 4 position, and the intensity of the effect is related to the type of substituent on the phenyl, from the 2 position of the thiazolic nucleus

New N-(oxazolylmethyl)-thiazolidinedione Active against Candida albicans Biofilm: Potential Als Proteins Inhibitors

C. albicans is the most frequently occurring fungal pathogen, and is becoming an increasing public health problem, especially in the context of increased microbial resistance. This opportunistic pathogen is characterized by a versatility explained mainly by its ability to form complex biofilm structures that lead to enhanced virulence and antibiotic resistance. In this context, a review of the known C. albicans biofilm formation inhibitors were performed and a new N-(oxazolylmethyl)-thiazolidinedione scaffold was constructed. 16 new compounds were synthesized and characterized in order to confirm their proposed structures. A general antimicrobial screening against Gram-positive and Gram-negative bacteria, as well as fungi, was performed and revealed that the compounds do not have direct antimicrobial activity. The anti-biofilm activity evaluation confirmed the compounds act as selective inhibitors of C. albicans biofilm formation. In an effort to substantiate this biologic profile, we used in silico investigations which suggest that the compounds could act by binding, and thus obstructing the functions of, the C. albicans Als surface proteins, especially Als1, Als3, Als5 and Als6. Considering the well documented role of Als1 and Als3 in biofilm formation, our new class of compounds that target these proteins could represent a new approach in C. albicans infection prevention and management