101623-71-6Relevant articles and documents
Synthesis of a novel cyclic prodrug of S -allyl-glutathione able to attenuate LPS-induced ROS production through the inhibition of MAPK pathways in U937 cells
Patruno, Antonia,Fornasari, Erika,Di Stefano, Antonio,Cerasa, Laura S.,Marinelli, Lisa,Baldassarre, Leonardo,Sozio, Piera,Turkez, Hasan,Franceschelli, Sara,Ferrone, Alessio,Di Giacomo, Viviana,Speranza, Lorenza,Felaco, Mario,Cacciatore, Ivana
, p. 66 - 74 (2015)
A novel cyclic prodrug of S-allyl-glutathione (CP11), obtained by using an acyloxy-alkoxy linker, was estimated for its pharmacokinetic and biological properties. The stability of CP11 was evaluated at pH 1.2, 7.4, in simulated fluids with different concentrations of enzymes, and in human plasma. The anti-inflammatory ability of CP11 was assessed in U937 cells, an immortalized human monocyte cell line. Results showed that CP11 is stable at acidic pH showing a possible advantage for oral delivery due to the longer permanence in the stomach. Having a permeability coefficient of 2.49 × 10-6 cm s-1, it was classified as discrete BBB-permeable compound. Biological studies revealed that CP11 is able to modulate inflammation mediated by LPS in U937 cells preventing the increase of ROS intracellular levels through interaction with the MAPK pathway.
Macrocyclic prodrugs of a selective nonpeptidic direct thrombin inhibitor display high permeability, efficient bioconversion but low bioavailability
Andersson, Vincent,Bergstr?m, Fredrik,Br?nalt, Jonas,Gr?nberg, Gunnar,Gustafsson, David,Karlsson, Staffan,Polla, Magnus,Bergman, Joakim,Kihlberg, Jan
, p. 6658 - 6670 (2016/08/05)
The only oral direct thrombin inhibitors that have reached the market, ximelagatran and dabigatran etexilat, are double prodrugs with low bioavailability in humans. We have evaluated an alternative strategy: the preparation of a nonpeptidic, polar direct
(3S,11aR)-6-[(phenylmethyl)oxy]-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-9 and/or (3S,11aR)-6-[(phenymethyl)oxy]-8-bromo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-10
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, (2016/01/20)
The compounds are intermediates in the preparation of therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are (3S,11aR)-6-[(phenylmethyl)oxy]-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-9 and/or (3S,11aR)-6-[(phenylmethyl)oxy]-8-bromo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-10.