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PDBsum entry 2bbb
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References listed in PDB file
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Key reference
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Title
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Design, Synthesis, And biological evaluation of monopyrrolinone-Based HIV-1 protease inhibitors possessing augmented p2' Side chains.
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Authors
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A.B.Smith,
A.K.Charnley,
H.Harada,
J.J.Beiger,
L.D.Cantin,
C.S.Kenesky,
R.Hirschmann,
S.Munshi,
D.B.Olsen,
M.W.Stahlhut,
W.A.Schleif,
L.C.Kuo.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
859-863.
[DOI no: ]
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PubMed id
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Abstract
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A series of monopyrrolinone-based HIV-1 protease inhibitors possessing
rationally designed P2' side chains have been synthesized and evaluated for
activity against wild-type HIV-1 protease. The most potent inhibitor displays
subnanomolar potency in vitro for the wild-type HIV-1 protease. Additionally,
the monopyrrolinone inhibitors retain potency in cellular assays against
clinically significant mutant forms of the virus. X-ray structures of these
inhibitors bound in the wild-type enzyme reveal important insights into the
observed biological activity.
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