17694-68-7Relevant articles and documents
Synthesis, structures, and biological activities of new 1H-1,2,4-triazole derivatives containing pyridine unit
Liu, Jian-Bing,Tao, Wei-Feng,Dai, Hong,Jin, Zhong,Fang, Jian-Xin
, p. 376 - 380 (2007)
Fourteen new 1H-1,2,4-triazole derivatives containing pyridine moiety were synthesized by condensation of 1-(pyridine-3-yl)-2-(1H-1,2,4-triazol1-yl) ethanone with aryl aldehydes, and their reaction conditions were studied. The title compounds were screened for their antibacterial and plant growth regulatory activities. The screening data revealed that most of the compounds showed some antifungal and plant growth regulatory activities.
Thiazole analogues of the marine alkaloid nortopsentin as inhibitors of bacterial biofilm formation
Carbone, Anna,Cascioferro, Stella,Parrino, Barbara,Carbone, Daniela,Pecoraro, Camilla,Schillaci, Domenico,Cusimano, Maria Grazia,Cirrincione, Girolamo,Diana, Patrizia
, (2021/02/02)
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 μM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
Synthesis, antioxidant and antimicrobial properties of novel pyridyl-carbonyl thiazoles as dendrodoine analogs
?ahin, Zafer,Biltekin, Sevde Nur,Yurtta?, Leyla,Demirayak, ?eref
, p. 1733 - 1741 (2021/01/04)
Marine compound dendrodoine was first obtained from tunicate species (Dendrodo grossularia). It has a five-membered ring, namely, it is a heterocycle thiadiazole, which is found rarely in natural sources. Following its biological activities, novel analogs have been investigated recently. Synthesis of the analogs for this study is realized with uncommon thiazole closure, including methylene-carbonyl condensation. Structures are elucidated by NMR (1H, 13C) and HRMS spectrums. As an alkaloid derivative, antioxidant properties were evaluated with DPPH and FRAP assays and antimicrobial effect with microdilution method. Among the series, 3bc-3cf showed higher antioxidant activity than those having 3 or 4-pyridyl substituents. There is lesser activity for 2-pyridyl activity for 2-pyridyl containing group, which may be a result of intramolecular interactions. No activity was observed against gram-negative bacteria at 250 μg/mL. 3ae and 3ce showed activity at 64 μg/mL against S. aureus and 3ae showed activity at 16 μg/mL against S. epidermidis gram-positive bacteria. Chloramphenicol showed activity against all microorganisms at 8-16 μg/mL. Sixteen original dendrodoine analogs have been defined by close/higher activity compared to dendrodoine analogs and Trolox.
