2j4i: Difference between revisions

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==Overview==
==Overview==
Structure-based drug design was exploited in the synthesis of, 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa), inhibitors, incorporating an alanylamide P4 group with acyclic tertiary, amide termini. Optimized hydrophobic contacts of one amide substituent in, P4 were complemented by hydrophobicity-modulating features in the second, producing potent fXa inhibitors including examples with excellent, anticoagulant properties.
Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group with acyclic tertiary amide termini. Optimized hydrophobic contacts of one amide substituent in P4 were complemented by hydrophobicity-modulating features in the second, producing potent fXa inhibitors including examples with excellent anticoagulant properties.


==Disease==
==Disease==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Protein complex]]
[[Category: Borthwick, A.D.]]
[[Category: Borthwick, A D.]]
[[Category: Brown, D.]]
[[Category: Brown, D.]]
[[Category: Campbell, M.]]
[[Category: Campbell, M.]]
[[Category: Chan, C.]]
[[Category: Chan, C.]]
[[Category: Convery, M.A.]]
[[Category: Convery, M A.]]
[[Category: Crowe, M.C.]]
[[Category: Crowe, M C.]]
[[Category: Dayal, S.]]
[[Category: Dayal, S.]]
[[Category: Diallo, H.]]
[[Category: Diallo, H.]]
[[Category: Kelly, H.A.]]
[[Category: Kelly, H A.]]
[[Category: King, N.Paul.]]
[[Category: King, N Paul.]]
[[Category: Kleanthous, S.]]
[[Category: Kleanthous, S.]]
[[Category: Kurtis, C.L.]]
[[Category: Kurtis, C L.]]
[[Category: Mason, A.M.]]
[[Category: Mason, A M.]]
[[Category: Mordaunt, J.E.]]
[[Category: Mordaunt, J E.]]
[[Category: Patel, C.]]
[[Category: Patel, C.]]
[[Category: Pateman, A.J.]]
[[Category: Pateman, A J.]]
[[Category: Senger, S.]]
[[Category: Senger, S.]]
[[Category: Shah, G.P.]]
[[Category: Shah, G P.]]
[[Category: Smith, P.W.]]
[[Category: Smith, P W.]]
[[Category: Watson, N.S.]]
[[Category: Watson, N S.]]
[[Category: Weston, H.E.]]
[[Category: Weston, H E.]]
[[Category: Young, R.J.]]
[[Category: Young, R J.]]
[[Category: Zhou, P.]]
[[Category: Zhou, P.]]
[[Category: CA]]
[[Category: CA]]
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[[Category: zymogen]]
[[Category: zymogen]]


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