724742-77-2Relevant academic research and scientific papers
Br?nsted acid-promoted thiazole synthesis under metal-free conditions using sulfur powder as the sulfur source
Ni, Penghui,Tan, Jing,Li, Rong,Huang, Huawen,Zhang, Feng,Deng, Guo-Jun
, p. 3931 - 3935 (2020/02/04)
A Br?nsted acid-promoted sulfuration/annulation reaction for the one-pot synthesis of bis-substituted thiazoles from benzylamines, acetophenones, and sulfur powder has been developed. One C-N bond and multi C-S bonds were selectively formed in one pot. The choice of the Br?nsted acid was the key to the high efficiency of this transformation under metal-free conditions.
New 2-phenylthiazoles as potential sortase a inhibitors: Synthesis, biological evaluation and molecular docking
Oniga, Smaranda Dafina,Araniciu, Catalin,Palage, Mariana Doina,Popa, Marcela,Chifiriuc, Mariana Carmen,Marc, Gabriel,Pirnau, Adrian,Stoica, Cristina Ioana,Lagoudis, Ioannis,Dragoumis, Theodoros,Oniga, Ovidiu
, (2017/11/21)
Sortase A inhibition is a well establish strategy for decreasing bacterial virulence by affecting numerous key processes that control biofilm formation, host cell entry, evasion and suppression of the immune response and acquisition of essential nutrients. A meta-analysis of structures known to act as Sortase A inhibitors provided the starting point for identifying a new potential scaffold. Based on this template a series of new potential Sortase A inhibitors, that contain the 2-phenylthiazole moiety, were synthesized. The physicochemical characterisation confirmed the identity of the proposed structures. Antibacterial activity evaluation showed that the new compounds have a reduced activity against bacterial cell viability. However, the compounds prevent biofilm formation at very low concentrations, especially in the case of E. faecalis. Molecular docking studies performed estimate that this is most likely due to the inhibition of Sortase A. The new compounds could be used as add-on therapies together with known antibacterial agents in order to combat multidrug-resistance enterococcal infections.
Synthesis and Antimicrobial Evaluation of Some New 4,5′-Bisthiazoles
Rozsa, Tibor,Duma, Mihaela,Vlase, Laurian,Ionu?, Ioana,P?rn?u, Adrian,Tiperciuc, Br?ndu?a,Oniga, Ovidiu
, p. 999 - 1006 (2015/08/06)
Thiazole and bisthiazole derivatives represent a prevalent scaffold in the antimicrobial drug discovery. Therefore, we have decided to synthesize some new series of 4,5′-bisthiazoles. A total of 17 compounds were synthesized, their structural elucidation
