54543-39-4Relevant academic research and scientific papers
Antibacterial activity of fluorobenzoylthiosemicarbazides and their cyclic analogues with 1,2,4-triazole scaffold
Kosikowska, Urszula,P?onka, Wojciech,Paneth, Agata,Paneth, Piotr,Trotsko, Nazar,Wujec, Monika
, (2021/05/28)
The development of drug-resistant bacteria is currently one of the major challenges in medicine. Therefore, the discovery of novel lead structures for the design of antibacterial drugs is urgently needed. In this structure–activity relationship study, a l
Discovery of protein-protein interaction inhibitors of replication protein A
Patrone, James D.,Kennedy, J. Phillip,Frank, Andreas O.,Feldkamp, Michael D.,Vangamudi, Bhavatarini,Pelz, Nicholas F.,Rossanese, Olivia W.,Waterson, Alex G.,Chazin, Walter J.,Fesik, Stephen W.
, p. 601 - 605 (2013/07/26)
Replication protein A (RPA) is a ssDNA binding protein that is essential for DNA replication and repair. The initiation of the DNA damage response by RPA is mediated by protein-protein interactions involving the N-terminal domain of the 70 kDa subunit with partner proteins. Inhibition of these interactions increases sensitivity toward DNA damage and replication stress and may therefore be a potential strategy for cancer drug discovery. Toward this end, we have discovered two lead series of compounds, derived from hits obtained from a fragment-based screen, that bind to RPA70N with low micromolar affinity and inhibit the binding of an ATRIP-derived peptide to RPA. These compounds may offer a promising starting point for the discovery of clinically useful RPA inhibitors.
Preparation and antiarthritic activity of new 1,5-diaryl-3-alkylthio-1H-1,2,4-triazoles and corresponding sulfoxides and sulfones
Szilagyi, Geza,Somorai, Tamas,Bozo, Eva,Lango, Jozsef,Nagy, Gabor,et al.
, p. 95 - 101 (2007/10/02)
A series of 1,5-diaryl-3-alkylthio-1H-1,2,4-triazoles and corresponding sulfoxides and sulfones was synthesized and evaluated as antiinflammatory agents in the rat adjuvant induced arthritis assay.Several analogues were found to be more potent than phenyl
