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7-Azabicycloheptane carboxylic acid: a proline replacement in a boroarginine thrombin inhibitor
W Han1, J C Pelletier, L J Mersinger
1Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Experimental Station, Wilmington, Delaware 19880, USA. wei.han@dupontpharma.com
Organic Letters
|June 3, 2000
Abstract:
[formula: see text] The synthesis of thrombin inhibitor 3, which incorporates conformationally constrained 7-azabicycloheptane carboxylic acid (1) as a proline replacement, is described. The inhibition constant (Ki(thrombin) = 2.9 nM) indicates that 1 is a reasonable replacement of proline in the formation of a beta-turn tripeptide mimetic.