2feq: Difference between revisions

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==Overview==

The synthesis and SAR of novel nanomolar thrombin inhibitors with the, common backbone, HOOC-CH(2)-d-cyclohexylalanyl-3,4-dehydroprolyl-NH-CH(2)-aryl-C(=NH)NH(2), are described together with their ecarin clotting time (ECT) prolongation, as measure for thrombin inhibition ex vivo. The aryl P1-moiety mimicking, the arginine part of the d-Phe-Pro-Arg derived thrombin inhibitors turned, out to be a key component for in vitro potency and in vivo activity., Optimization of this part led to compounds with improved antithrombin, activity in rats and dogs after oral administration compared to the, recently launched anticoagulant melagatran.

The synthesis and SAR of novel nanomolar thrombin inhibitors with the common backbone HOOC-CH(2)-d-cyclohexylalanyl-3,4-dehydroprolyl-NH-CH(2)-aryl-C(=NH)NH(2) are described together with their ecarin clotting time (ECT) prolongation as measure for thrombin inhibition ex vivo. The aryl P1-moiety mimicking the arginine part of the d-Phe-Pro-Arg derived thrombin inhibitors turned out to be a key component for in vitro potency and in vivo activity. Optimization of this part led to compounds with improved antithrombin activity in rats and dogs after oral administration compared to the recently launched anticoagulant melagatran.

==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: 34P]]

[[Category: thrombin inhibitor]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:20:46 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-The synthesis and SAR of novel nanomolar thrombin inhibitors with the, common backbone, HOOC-CH(2)-d-cyclohexylalanyl-3,4-dehydroprolyl-NH-CH(2)-aryl-C(=NH)NH(2), are described together with their ecarin clotting time (ECT) prolongation, as measure for thrombin inhibition ex vivo. The aryl P1-moiety mimicking, the arginine part of the d-Phe-Pro-Arg derived thrombin inhibitors turned, out to be a key component for in vitro potency and in vivo activity., Optimization of this part led to compounds with improved antithrombin, activity in rats and dogs after oral administration compared to the, recently launched anticoagulant melagatran.
+The synthesis and SAR of novel nanomolar thrombin inhibitors with the common backbone HOOC-CH(2)-d-cyclohexylalanyl-3,4-dehydroprolyl-NH-CH(2)-aryl-C(=NH)NH(2) are described together with their ecarin clotting time (ECT) prolongation as measure for thrombin inhibition ex vivo. The aryl P1-moiety mimicking the arginine part of the d-Phe-Pro-Arg derived thrombin inhibitors turned out to be a key component for in vitro potency and in vivo activity. Optimization of this part led to compounds with improved antithrombin activity in rats and dogs after oral administration compared to the recently launched anticoagulant melagatran.
 ==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: 34P]]
 [[Category: thrombin inhibitor]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:25:02 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:20:46 2008''