24010-80-8Relevant articles and documents
In Vitro and in Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas
Ottavi, Samantha,Scarry, Sarah M.,Mosior, John,Ling, Yan,Roberts, Julia,Singh, Amrita,Zhang, David,Goullieux, Laurent,Roubert, Christine,Bacqué, Eric,Lagiakos, H. Rachel,Vendome, Jeremie,Moraca, Francesca,Li, Kelin,Perkowski, Andrew J.,Ramesh, Remya,Bowler, Matthew M.,Tracy, William,Feher, Victoria A.,Sacchettini, James C.,Gold, Ben S.,Nathan, Carl F.,Aubé, Jeffrey
supporting information, p. 1996 - 2022 (2022/01/31)
A newly validated target for tuberculosis treatment is phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. The structure-activity relat
3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer's Disease
Prati, Federica,De Simone, Angela,Armirotti, Andrea,Summa, Maria,Pizzirani, Daniela,Scarpelli, Rita,Bertozzi, Sine Mandrup,Perez, Daniel I.,Andrisano, Vincenza,Perez-Castillo, Ana,Monti, Barbara,Massenzio, Francesca,Polito, Letizia,Racchi, Marco,Sabatino, Piera,Bottegoni, Giovanni,Martinez, Ana,Cavalli, Andrea,Bolognesi, Maria L.
, p. 1665 - 1682 (2015/11/09)
One of the main obstacles toward the discovery of effective anti-Alzheimer drugs is the multifactorial nature of its etiopathology. Therefore, the use of multitarget-directed ligands has emerged as particularly suitable. Such ligands, able to modulate different neurodegenerative pathways, for example, amyloid and tau cascades, as well as cognitive and neurogenic functions, are fostered to come. In this respect, we report herein on the first class of BACE-1/GSK-3β dual inhibitors based on a 3,4-dihydro-1,3,5-triazin-2(1H)-one skeleton, whose hit compound 1 showed interesting properties in a preliminary investigation. Notably, compound 2, endowed with well-balanced potencies against the two isolated enzymes (IC50 of 16 and 7 μM against BACE-1 and GSK-3β, respectively), displayed effective neuroprotective and neurogenic activities and no neurotoxicity in cell-based assays. It also showed good brain permeability in a pharmacokinetic assessment in mice. Overall, triazinone derivatives, thanks to the simultaneous modulation of multiple points of the diseased network, might emerge as suitable candidates to be tested in in vivo Alzheimer's disease models.
Synthesis of novel 4,6-di(substituted)amino- 1,2-dihydro-1,3,5-triazine derivatives as topical antiseptic agents
Maeda, Shirou,Kita, Toshiko,Meguro, Kanji
supporting information; experimental part, p. 597 - 600 (2009/11/30)
A series of novel 4,6-di(substituted)arnino-1,2-dihydro-1,3,5- triazine derivatives designed to have ClogP of 5.1-7.5 was synthesized and evaluated for their antiseptic properties by MIC and MBC tests against Gram-positive and Gram-negative bacteria, incl