193964-28-2Relevant academic research and scientific papers
Antithrombotic diamines
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, (2012/10/23)
This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 2. Exploring interactions at the proximal (S2) binding site
Sall, Daniel J.,Briggs, Stephen L.,Chirgadze, Nickolay Y.,Clawson, David K.,Gifford-Moore, Donetta S.,Klimkowski, Valentine J.,McCowan, Jefferson R.,Smith, Gerald F.,Wikel, James H.
, p. 2527 - 2532 (2007/10/03)
In an effort to increase the thrombin inhibitory activity of a novel series of inhibitors (i.e., 1a), substituents were incorporated at the C-3' position of the C-3 aryl ring (2). Consistent with the X-ray crystallography studies, small hydrophobic groups at the C-3' site (Br and Me) enhanced thrombin inhibitory activity by 8-fold. However, a few more hydrophilic substituents (NO2 and OMe) also enhanced the potency of the series. The biological results are discussed in terms of molecular modeling studies.
