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- W1974632012 abstract "SSR182289A 1 is the result of a rational optimisation process leading to an orally active thrombin inhibitor. The structure incorporates an original 2-(acetylamino)-[1,1'-biphenyl]-3-sulfonyl N-terminal motif, a central l-Arg surrogate carrying a weakly basic 3-amino-pyridine, and an unusual 4-difluoropiperidine at the C-terminus. Its synthesis is convergent and palladium catalysis has been employed for the construction of the key C-C bonds: Suzuki coupling for the bis-aryl fragment and Sonogashira reaction for the delta- bond of the central amino-acid chain. The compound is a potent inhibitor of thrombin's activities in vitro and demonstrates potent oral anti-thrombotic potencies in three rat models of thrombosis. The observed in vitro potency could be rationalized through the examination of the interactions within the SSR182289A 1 - thrombin crystal structure. SSR182289A 1, has been therefore selected for further development." @default.
- W1974632012 created "2016-06-24" @default.
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- W1974632012 date "2004-04-01" @default.
- W1974632012 modified "2023-10-16" @default.
- W1974632012 title "SSR182289A, a selective and potent orally active thrombin inhibitor" @default.
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- W1974632012 doi "https://doi.org/10.1016/j.bmc.2004.01.016" @default.
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