2pr3: Difference between revisions

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==Overview==

A novel series of pyrrolidine-1,2-dicarboxamides was discovered as factor, Xa inhibitors using structure-based drug design. This series consisted of, a neutral 4-chlorophenylurea P1, a biphenylsulfonamide P4 and a D-proline, scaffold (1, IC(50) = 18 nM). Optimization of the initial hit resulted in, an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) =, 0.38 nM), which was shown to be efficacious in a canine electrolytic model, of thrombosis with minimal bleeding.

A novel series of pyrrolidine-1,2-dicarboxamides was discovered as factor Xa inhibitors using structure-based drug design. This series consisted of a neutral 4-chlorophenylurea P1, a biphenylsulfonamide P4 and a D-proline scaffold (1, IC(50) = 18 nM). Optimization of the initial hit resulted in an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) = 0.38 nM), which was shown to be efficacious in a canine electrolytic model of thrombosis with minimal bleeding.

==Disease==

Known disease associated with this structure: Factor X deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227600 227600]]

==About this Structure==

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[[Category: Homo sapiens]]

[[Category: Protein complex]]

[[Category: Bigge, C.F.]]

[[Category: Bigge, C F.]]

[[Category: Finzel, B.C.]]

[[Category: Finzel, B C.]]

[[Category: Kohrt, J.T.]]

[[Category: Kohrt, J T.]]

[[Category: Zhang, E.]]

[[Category: 237]]

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[[Category: fxa coagulation factor inhibitor]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:32:12 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-A novel series of pyrrolidine-1,2-dicarboxamides was discovered as factor, Xa inhibitors using structure-based drug design. This series consisted of, a neutral 4-chlorophenylurea P1, a biphenylsulfonamide P4 and a D-proline, scaffold (1, IC(50) = 18 nM). Optimization of the initial hit resulted in, an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) =, 0.38 nM), which was shown to be efficacious in a canine electrolytic model, of thrombosis with minimal bleeding.
+A novel series of pyrrolidine-1,2-dicarboxamides was discovered as factor Xa inhibitors using structure-based drug design. This series consisted of a neutral 4-chlorophenylurea P1, a biphenylsulfonamide P4 and a D-proline scaffold (1, IC(50) = 18 nM). Optimization of the initial hit resulted in an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) = 0.38 nM), which was shown to be efficacious in a canine electrolytic model of thrombosis with minimal bleeding.
+==Disease==
+Known disease associated with this structure: Factor X deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227600 227600]]
 ==About this Structure==
@@ Line 14: / Line 17: @@
 [[Category: Homo sapiens]]
 [[Category: Protein complex]]
-[[Category: Bigge, C.F.]]
+[[Category: Bigge, C F.]]
-[[Category: Finzel, B.C.]]
+[[Category: Finzel, B C.]]
-[[Category: Kohrt, J.T.]]
+[[Category: Kohrt, J T.]]
 [[Category: Zhang, E.]]
 [[Category: 237]]
@@ Line 23: / Line 26: @@
 [[Category: fxa coagulation factor inhibitor]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:37:29 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:32:12 2008''