2199-89-5Relevant articles and documents
Coumarin derivatives act as novel inhibitors of human dipeptidyl peptidase III: Combined in vitro and in silico study
?ubari?, Domagoj,Agi?, Dejan,Be?lo, Drago,Kara?i?, Zrinka,Karna?, Maja,Lisjak, Miroslav,Lon?ari?, Melita,Molnar, Maja,Popovi?, Boris M.,Rastija, Vesna,Tomi?, Sanja
, (2021/06/22)
Dipeptidyl peptidase III (DPP III), a zinc-dependent exopeptidase, is a member of the metalloproteinase family M49 with distribution detected in almost all forms of life. Although the physiological role of human DPP III (hDPP III) is not yet fully elucida
Copper(I)-promoted cycloalkylation-peroxidation of unactivated alkenes via sp3 C-H functionalisation
Banerjee, Arghya,Santra, Sourav Kumar,Mishra, Aniket,Khatun, Nilufa,Patel, Bhisma K.
supporting information, p. 1307 - 1312 (2015/01/30)
A copper(i)-promoted cycloalkylation-peroxidation strategy has been developed via a three-component reaction involving cycloalkanes, tert-butyl hydroperoxide (TBHP) and internal conjugated alkenes possessing electron-withdrawing groups (EWGs). This process installs C-O and C-C bonds via sp3 C-H functionalisation with concomitant generation of two stereocentres. This regioselective radical addition of coumarin system is opposite to that of styrene.
New coumarin derivatives: Design, synthesis and use as inhibitors of hMAO
He, Xu,Chen, Yan-Yan,Shi, Jing-Bo,Tang, Wen-Jiang,Pan, Zhi-Xiang,Dong, Zhi-Qiang,Song, Bao-An,Li, Jun,Liu, Xin-Hua
, p. 3732 - 3738 (2014/07/07)
A series new 2H-chromene-3-carboxamides (4a-4i) and S-2H-chromene-3- carbothioates (5j-5t) were synthesized and evaluated as monoamine oxidase A and B inhibitors. Among them, compound 5k (IC50 = 0.21 μM, IC 50 iproniazid = 7.65 μM) showed the most activity and higher MAO-B selectivity (189.2-fold vs 1-fold) with respect to the MAO-A isoform. The need to clarify at a 3D level some important molecular aspects of discussed SAR, we undertaked a number of docking simulations to better assess. The steric effect was analyzed interms of both posing and scoring by investigating the nature of the binding interactions. The docking results of active compound 5k with hMAO-B complex indicated that conserved residue ILE 199 was important for ligand binding via Sigma-Pi interaction.