Key result
Novel thienothiophene α-sulfonamides potently inhibit platelet aggregation in vivo via IV and oral dosing.
Centrally constrained thienothiophene α-sulfonamides demonstrate potent, long-acting in vivo inhibition of platelet aggregation at microgram per kilogram dosing.
Hypothesis-generating for oral GPIIb/IIIa inhibitors; leaves open human translation and safety.
Centrally Constrained Thienothiophene R-Sulfonamides Are Potent, Long Acting in Vivo Inhibitors of Platelet Aggregation.Page 2409.In the Abstract, line 8, mg/kg should be µg/kg: ...an iv dose of 5 µg/kg, and an oral dose of 50-90 µg/kg followed by low daily doses of 10 µg/kg...
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Egbertson et al. (1999) studied this question. Centrally constrained thienothiophene α-sulfonamides are potent, long-acting in vivo inhibitors of platelet aggregation at doses of 5 µg/kg IV and 50-90 µg/kg orally.
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