2a4f: Difference between revisions
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'''Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.'''<br /> | '''Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.'''<br /> | ||
==Overview== | ==Overview== | ||
As part of our efforts to identify potent HIV-1 protease inhibitors that | As part of our efforts to identify potent HIV-1 protease inhibitors that are active against resistant viral strains, structural modification of the azacyclic urea (I) was undertaken by incorporating acyl groups as P(1)' ligands. The extensive SAR study has yielded a series of N-acyl azacyclic ureas (II), which are highly potent against both wild-type and multiple PI-resistant viral strains. | ||
==About this Structure== | ==About this Structure== | ||
2A4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with AAU as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http:// | 2A4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=AAU:'>AAU</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/HIV-1_retropepsin HIV-1 retropepsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.16 3.4.23.16] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2A4F OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Saldivar, A.]] | [[Category: Saldivar, A.]] | ||
[[Category: Sham, H.]] | [[Category: Sham, H.]] | ||
[[Category: Stewart, K | [[Category: Stewart, K D.]] | ||
[[Category: Stoll, V.]] | [[Category: Stoll, V.]] | ||
[[Category: Sun, M.]] | [[Category: Sun, M.]] | ||
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[[Category: hiv protease]] | [[Category: hiv protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:23:34 2008'' | ||
Revision as of 17:23, 21 February 2008
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Synthesis and Activity of N-Axyl Azacyclic Urea HIV-1 Protease Inhibitors with High Potency Against Multiple Drug Resistant Viral Strains.
OverviewOverview
As part of our efforts to identify potent HIV-1 protease inhibitors that are active against resistant viral strains, structural modification of the azacyclic urea (I) was undertaken by incorporating acyl groups as P(1)' ligands. The extensive SAR study has yielded a series of N-acyl azacyclic ureas (II), which are highly potent against both wild-type and multiple PI-resistant viral strains.
About this StructureAbout this Structure
2A4F is a Single protein structure of sequence from Human immunodeficiency virus 1 with as ligand. Active as HIV-1 retropepsin, with EC number 3.4.23.16 Full crystallographic information is available from OCA.
ReferenceReference
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains., Zhao C, Sham HL, Sun M, Stoll VS, Stewart KD, Lin S, Mo H, Vasavanonda S, Saldivar A, Park C, McDonald EJ, Marsh KC, Klein LL, Kempf DJ, Norbeck DW, Bioorg Med Chem Lett. 2005 Dec 15;15(24):5499-503. Epub 2005 Oct 3. PMID:16203141
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