1.
Chembiochem
; 14(18): 2413-7, 2013 Dec 16.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24174158
Asunto(s)
Antígenos Bacterianos/inmunología , Glucolípidos/inmunología , Mycobacterium tuberculosis/inmunología , Vacunas contra la Tuberculosis/inmunología , Tuberculosis/prevención & control , Antígenos Bacterianos/química , Glucolípidos/química , Humanos , Mycobacterium tuberculosis/química , Trehalosa , Tuberculosis/inmunología , Tuberculosis/microbiología , Vacunas contra la Tuberculosis/química
2.
J Med Chem
; 57(17): 7293-316, 2014 Sep 11.
Artículo
en Inglés
| MEDLINE
| ID: mdl-25075638
RESUMEN
In the search of a potential backup for clopidogrel, we have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, we report here the main steps of the optimization process leading to the identification of the preclinical candidate SAR216471. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. SAR216471 displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents.