1242283-93-7Relevant academic research and scientific papers
Discovery and development of substituted thiadiazoles as inhibitors of Staphylococcus aureus Sortase A
Wehrli, Patrick M.,Uzelac, Ivana,Olsson, Thomas,Jacso, Tomas,Tietze, Daniel,Gottfries, Johan
, (2019/08/16)
High-throughput screening of small-molecule libraries has led to the identification of thiadiazoles as a new class of inhibitors against Staphylococcus aureus sortase A (SrtA). N-(5-((4-nitrobenzyl)thio)-1,3,4-thiadiazol-2-yl)nicotinamide (IC50
Design and synthesis of thiadiazoles and thiazoles targeting the Bcr-Abl T315I mutant: From docking false positives to ATP-noncompetitive inhibitors
Radi, Marco,Crespan, Emmanuele,Falchi, Federico,Bernardo, Vincenzo,Zanoli, Samantha,Manetti, Fabrizio,Schenone, Silvia,Maga, Giovanni,Botta, Maurizio
scheme or table, p. 1226 - 1231 (2011/02/21)
(Figure Presented) Overcoming resistance: In an effort to optimize our previously identified dual Src/Abl hits, a new series of 1,3,4-thiadiazoles and 1,3-thiazoles were designed and synthesized, paying particular attention to the reduction of their lipophilicity and to the improvement of the affinity towards the drug-resistant T315I mutant. Compound 5 was identified as a promising allosteric inhibitor of the T315I mutant.
