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A new series of synthetic thrombin-inhibitors (OM-inhibitors) having extremely potent and selective action

โœ Scribed by S. Okamoto; A. Hijikata; K. Ikezawa; K. Kinjo; R. Kikumoto; S. Tonomura; Y. Tamao


Book ID
119033312
Publisher
Elsevier Science
Year
1976
Tongue
English
Weight
406 KB
Volume
8
Category
Article
ISSN
0049-3848

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Amidinohydrazones as guanidine bioisoste
โœ Richard M. Soll; Tianobao Lu; Bruce Tomczuk; Carl R. Illig; Cynthia Fedde; Steph ๐Ÿ“‚ Article ๐Ÿ“… 2000 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 228 KB

We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a non-peptide scaffold. Compound 4 exhibits nM inhibition of thrombin, is selective for thrombin, and shows 60 and 23% bioavailability in rabbits a