ABSTRACT
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.
Subject(s)
Anti-Infective Agents/chemistry , Small Molecule Libraries/chemistry , Triazenes/chemistry , Candida albicans/drug effects , Drug Evaluation, Preclinical , Enterococcus faecalis/drug effects , Escherichia coli/drug effects , Microbial Sensitivity Tests , Molecular Structure , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects , Structure-Activity Relationship , Triazenes/pharmacologyABSTRACT
Objective:To evaluate the total phenolic contents,antioxidant and antigiycation activities of leaves,barks,roots and kernels from two cultiivars of Mangifera indica (Anacardiiaceae).Method:Total phenolic contents were determined by using Folin-Ciocalteu's method.The antioxidant activities were assessed by three different protocols including DPPH,oxygen radical absorbance capacity and iron (Ⅱ) chelation assays.In addition,in vitro bovine serum albumin/D-ribose assay was chosen to evaluate the antiglycation properties of the extracts.Results:All the investigated extracts were found to contain high level of total phenols as well as potent antioxidant activities.Kernel extracts showed the highest total phenol contents and DPPH radical scavenging activities whereas higher oxygen radical absorbance capacity values were observed for leave,root and bark extracts.Besides,extracts from leaves,roots and barks from both cultivars exhibited potent inhibitory effects against the formation of advanced glycation end products,with IC50 values lower than the standard positive control aminoguanidine.Conclusions:The potent antigiycation and antioxidative activities of these two Mangifera indica cultivars suggest a possible role in targeting aging,diabetic complications and oxidative stress related diseases.
ABSTRACT
A new class of anti-biofilm compounds possessing 1,4-disubstituted-(1H)-1,2,3-triazolic cores was designed. Their efficient synthesis was performed by means of click chemistry through 1,3-dipolar cycloadditions. Two compounds were found to act as specific anti-biofilm agents against a gram negative species.
Subject(s)
Anti-Bacterial Agents/therapeutic use , Biofilms/drug effects , Drug Delivery Systems , Drug Design , Terpenes/chemical synthesis , Bacteria/drug effects , Terpenes/chemistry , Terpenes/pharmacology , Triazoles/chemistryABSTRACT
A series of primaquine analogs was prepared, according to a conformationally restricted conformation of primaquine. In vitro antiplasmodial activities were evaluated and showed that all compounds were active on different strains of Plasmodium falciparum. In particular compounds 5 and 15 possessing a methoxy group were more active than was primaquine. Furthermore, analog 5 displayed good in vitro gametocytocidal activity. In addition selectivity indexes were calculated in respect with cytotoxic activities on Vero cell lines.
