Synthesis and Characterization of Novel Five-Membered Heterocycles and Their Activity against Candida Yeasts
摘要:
Some new tetrazole derivatives were prepared by the reaction between the prepared azomethine compounds I-6-I-10 with sodium azide in anhydrous tetrahydrofuran (THF) with a few drops of distilled water and under reflux conditions. Azomethine compounds were prepared by thermal condensation reactions of aromatic aldehydes with primary aromatic amines. The prepared compounds (tetrazole derivatives) were screened for their antibacterial activity (by disc diffusion method). Compound I-6 is the most active derivative that has recorded a significantly (p<0.01) stronger influence to inhibit the growth of Candida zeylanoides with an average zone of inhibition of 26.0 mm. Derivatives I-7 and I-9 showed the lowest zone of inhibition of 8.0 mm against Candida zeylanoides. This study may be helpful in designing more potential anticandidal agents for therapeutic use in the future.
From Dynamic Combinatorial Chemistry to in Vivo Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors
摘要:
The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, in vivo evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.
From Dynamic Combinatorial Chemistry to <i>in Vivo</i> Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors
作者:Jalal Soubhye、Michel Gelbcke、Pierre Van Antwerpen、François Dufrasne、Mokhtaria Yasmina Boufadi、Jean Nève、Paul G. Furtmüller、Christian Obinger、Karim Zouaoui Boudjeltia、Franck Meyer
DOI:10.1021/acsmedchemlett.6b00417
日期:2017.2.9
The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, in vivo evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.
Synthesis and Characterization of Novel Five-Membered Heterocycles and Their Activity against Candida Yeasts
作者:Hiba Maher Tawfeeq、Rasim Farraj Muslim、Obaid Hasan Abid、Mustafa Nadhim Owaid
DOI:10.17344/acsi.2018.4719
日期:——
Some new tetrazole derivatives were prepared by the reaction between the prepared azomethine compounds I-6-I-10 with sodium azide in anhydrous tetrahydrofuran (THF) with a few drops of distilled water and under reflux conditions. Azomethine compounds were prepared by thermal condensation reactions of aromatic aldehydes with primary aromatic amines. The prepared compounds (tetrazole derivatives) were screened for their antibacterial activity (by disc diffusion method). Compound I-6 is the most active derivative that has recorded a significantly (p<0.01) stronger influence to inhibit the growth of Candida zeylanoides with an average zone of inhibition of 26.0 mm. Derivatives I-7 and I-9 showed the lowest zone of inhibition of 8.0 mm against Candida zeylanoides. This study may be helpful in designing more potential anticandidal agents for therapeutic use in the future.