Abstract
Novel, highly selective and potent thrombin inhibitors were identified as a result of combing the 3-benzylsulfonylamino-2-pyridinone acetamide P(2)-P(3) surrogate with weakly basic partially saturated heterobicyclic P(1)-arginine mimetics 1-8. The design, synthesis, biological activity, and the binding modes of non-covalent thrombin inhibitors featuring P(1)-4,5,6,7-tetrahydroindazole, 5,6,7,8-tetrahydroquinazoline, and 4,5,6,7-tetrahydrobenzothiazole moieties are described.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemistry*
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Acetamides / pharmacology
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Antithrombins / chemistry*
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Antithrombins / pharmacology
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Arginine / chemistry*
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Arginine / pharmacology
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Humans
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Piperidones / chemistry*
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Piperidones / pharmacology
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Pyridones / chemistry*
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Pyridones / pharmacology
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Thrombin / antagonists & inhibitors
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Thrombin / chemistry
Substances
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3-aminopiperidine-2-one
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Acetamides
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Antithrombins
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Piperidones
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Pyridones
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Arginine
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Thrombin