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Active site-directed thrombin inhibitors--II. Studies related to arginine/guanidine bioisosteres. 1995
D R St Laurent, and
N Balasubramanian, and
W T Han, and
A Trehan, and
M E Federici, and
N A Meanwell, and
J J Wright, and
S M Seiler
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA.
A series of N-arylsulfonylarginine amides was synthesized wherein the guanidine or arginine moiety was isosterically replaced by a number of heterocyclic functionalities. These compounds were evaluated as potential active-site inhibitors of thrombin. Bisamidines 11a-n showed a similar SAR to that of simple arginine compounds. The ex vivo clotting time measurement of 11d after ip dosing showed prolongation of clotting time in rats.
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