2a2x: Difference between revisions

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==Overview==

Synthesis and SAR of orally active thrombin inhibitors of the, d-Phe-Pro-Arg type with focus on the P2-moiety are described. The, unexpected increase in in vitro potency, oral bioavailability, and in vivo, activity of inhibitors with dehydroproline as P2-isostere is discussed., Over a period of 24h the antithrombin activity of the most active, inhibitors with IC(50)s in the nanomolar range was determined in dogs, demonstrating high thrombin inhibitory activity in plasma and an, appropriate duration of action after oral administration.

Synthesis and SAR of orally active thrombin inhibitors of the d-Phe-Pro-Arg type with focus on the P2-moiety are described. The unexpected increase in in vitro potency, oral bioavailability, and in vivo activity of inhibitors with dehydroproline as P2-isostere is discussed. Over a period of 24h the antithrombin activity of the most active inhibitors with IC(50)s in the nanomolar range was determined in dogs demonstrating high thrombin inhibitory activity in plasma and an appropriate duration of action after oral administration.

==Disease==

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[[Category: Thrombin]]

[[Category: Baucke, D.]]

[[Category: Hoeffken, H.W.]]

[[Category: Hoeffken, H W.]]

[[Category: Hornberger, W.]]

[[Category: Lange, U.E.W.]]

[[Category: Lange, U E.W.]]

[[Category: Mack, H.]]

[[Category: Seitz, W.]]

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[[Category: serine protease]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Fri~~ Feb ~~15 17~~:13:54 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:23:03 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-Synthesis and SAR of orally active thrombin inhibitors of the, d-Phe-Pro-Arg type with focus on the P2-moiety are described. The, unexpected increase in in vitro potency, oral bioavailability, and in vivo, activity of inhibitors with dehydroproline as P2-isostere is discussed., Over a period of 24h the antithrombin activity of the most active, inhibitors with IC(50)s in the nanomolar range was determined in dogs, demonstrating high thrombin inhibitory activity in plasma and an, appropriate duration of action after oral administration.
+Synthesis and SAR of orally active thrombin inhibitors of the d-Phe-Pro-Arg type with focus on the P2-moiety are described. The unexpected increase in in vitro potency, oral bioavailability, and in vivo activity of inhibitors with dehydroproline as P2-isostere is discussed. Over a period of 24h the antithrombin activity of the most active inhibitors with IC(50)s in the nanomolar range was determined in dogs demonstrating high thrombin inhibitory activity in plasma and an appropriate duration of action after oral administration.
 ==Disease==
@@ Line 18: / Line 18: @@
 [[Category: Thrombin]]
 [[Category: Baucke, D.]]
-[[Category: Hoeffken, H.W.]]
+[[Category: Hoeffken, H W.]]
 [[Category: Hornberger, W.]]
-[[Category: Lange, U.E.W.]]
+[[Category: Lange, U E.W.]]
 [[Category: Mack, H.]]
 [[Category: Seitz, W.]]
@@ Line 27: / Line 27: @@
 [[Category: serine protease]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:13:54 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:23:03 2008''