21665-53-2Relevant academic research and scientific papers
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs
Tber, Zahira,Wartenberg, Mylène,Jacques, Jean-Eddy,Roy, Vincent,Lecaille, Fabien,Warszycki, Dawid,Bojarski, Andrzej J.,Lalmanach, Gilles,Agrofoglio, Luigi A.
, p. 4310 - 4319 (2018/07/30)
We report herein the synthesis and biological evaluation of a new series of 2,4,6-trisubstituted 1,3,5-triazines as reversible inhibitors of human cysteine cathepsins. The desired products bearing morpholine and N-Boc piperidine, respectively, were obtained in three to four steps from commercially available trichlorotriazine. Seventeen hitherto unknown compounds were evaluated in vitro against various cathepsins for their inhibitory properties. Among them, compound 7c (4-(morpholin-4-yl)-6-[4-(trifluoromethoxy)anilino]-1,3,5-triazine-2-carbonitrile) was identified as the most potent and selective inhibitor of cathepsin S (Ki = 2 ± 0.3 nM). Also 7c impaired the autocatalytic maturation of procathepsin S. Molecular docking studies support that 7c bound within the active site of cathepsin S, by interacting with Gly23, Cys25 and Trp26 (S1 subsite), with Asn67, Gly69 and Phe70 (S2 subsite) and with Gln19 (S1′ pocket).
Design and Development of Novel 4-(4-(1H-Tetrazol-5-yl)-1H-pyrazol-1-yl)-6-morpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine as Cardiotonic Agent via Inhibition of PDE3
Mao, Zhi-Wei,Li, Qiao-Ling,Wang, Ping,Sun, Yang-Li,Liu, Yu
, p. 268 - 276 (2016/04/26)
The classical phosphodiesterase 3A (PDE3A) inhibitors provide relaxation of the vasculature system via increasing the cellular level of cyclic adenosine monophosphate (cAMP) and proved to be useful in the management of congestive heart failure. Consequent
