338462-91-2Relevant academic research and scientific papers
HIV protease inhibiting compounds
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Page/Page column 145, (2010/02/12)
A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Stereoselective synthesis of photoreactive peptidomimetic γ-secretase inhibitors
Chun, Jiong,Yin, Ye Ingrid,Yang, Guangli,Tarassishin, Leonid,Li, Yue-Ming
, p. 7344 - 7347 (2007/10/03)
The first asymmetric synthesis of novel, potent photoreactive γ-secretase inhibitors 2 and 3 has been accomplished. Two Stereoselective methods for the preparation of lactone 9 are described. Protected benzophenone intermediate 19 is prepared via an aldol-elimination reaction followed by a PtO2-catalyzed asymmetric hydrogenation. Two routes leading from 19 to compounds 2 and 3 are evaluated. The application of 3 as an activity-based probe has been demonstrated by localizing γ-secretase activity in the plasma membrane of intact cells.
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1'phenyl substituents: X-ray crystal structure assisted design
Thompson,Fitzgerald,Holloway,Emini,Darke,McKeever,Schleif,Quintero,Zugay,Tucker,Schwering,Homnick,Nunberg,Springer,Huff
, p. 1685 - 1701 (2007/10/02)
By tethering of a polar hydrophilic group to the P1 or P1' substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved. The optimum enhancement of anti-HIV activity was observed with the 4-morpholinylethoxy substituent. The substituent effect is consistent with a model derived from inhibitor docked in the crystal structure of the native enzyme. An X-ray crystal structure of the inhibited enzyme determined to 2.25 A verifies the modeling predictions.
A Stereocontrolled Synthesis of Hydroxyethylene Dipeptide Isosteres Using Novel, Chiral Aminoalkyl Epoxides and γ-(Aminoalkyl) γ-Lactones
Evans, Ben E.,Rittle, Kenneth E.,Homnick, Carl F.,Springer, James P.,Hirshfield, Jordan,Veber, Daniel F.
, p. 4615 - 4625 (2007/10/02)
A stereocontrolled synthesis of the hydroxyethylene dipeptide isosteric unit 1 is described.This synthesis is capable of providing all eight stereoisomers of 1 and is amenable to variation of substituents R1 and R2.Also described are the novel chiral epoxides 2 and substituted γ-lactones 3, key intermediates in this synthesis having potentially broad application.
