126410-53-5Relevant academic research and scientific papers
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.
HIV protease inhibitors useful for the treatment of aids
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, (2008/06/13)
[From equivalent EP0434365A2] Compounds of the form, A-G-B-B-J wherein A is an amine protecting group or urethane, G a dipeptide isostere substituted with a basic amine nitrogen, B an amino acid or analog thereof, and J a small terminal group are describe
