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1.
Chem Commun (Camb) ; 53(20): 2962-2965, 2017 Mar 07.
Article in English | MEDLINE | ID: mdl-28229136

ABSTRACT

A catalyst containing small (ca. 2.5 nm) and crystalline Pt nanoparticles embedded into the walls of a mesostructured silica framework was found to be highly active in alkene hydrosilylation reaching TONs of ca. 105. More importantly, no Pt leaching was detected. This result is remarkable because Pt leaching is a recurrent problem in alkene hydrosilylation, which often prevents heterogeneous catalysts from being used industrially. This result is in contrast to the significant Pt leaching observed for other Pt/SiO2 catalysts.

2.
Chem Commun (Camb) ; 51(90): 16194-6, 2015 Nov 21.
Article in English | MEDLINE | ID: mdl-26393811

ABSTRACT

Colloidal suspensions of monodisperse platinum nanoparticles of 2 nm diameter have been used to catalyze the hydrosilylation of 1-octene with a polymethylhydrosiloxane. The nanoparticles were found to be as efficient as Karstedt's complex, showing that colloid formation from homogeneous species during hydrosilylation reactions is not necessarily a deactivation pathway. These results also reactivated the debate on whether Karstedt's complex was truly homogeneous or colloidal during catalysis.

3.
J Med Chem ; 52(19): 5826-36, 2009 Oct 08.
Article in English | MEDLINE | ID: mdl-19791800

ABSTRACT

Protease activated receptors (PARs) or thrombin receptors constitute a class of G-protein-coupled receptors (GPCRs) implicated in the activation of many physiological mechanisms. Thus, thrombin activates many cell types such as vascular smooth muscle cells, leukocytes, endothelial cells, and platelets via activation of these receptors. In humans, thrombin-induced platelet aggregation is mediated by one subtype of these receptors, termed PAR1. This article describes the discovery of new antagonists of these receptors and more specifically two compounds: 2-[5-oxo-5-(4-pyridin-2-ylpiperazin-1-yl)penta-1,3-dienyl]benzonitrile 36 (F 16618) and 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone 39 (F 16357), obtained after optimization. Both compounds are able to inhibit SFLLR-induced human platelet aggregation and display antithrombotic activity in an arteriovenous shunt model in the rat after iv or oral administration. Furthermore, these compounds are devoid of bleeding side effects often observed with other types of antiplatelet drugs, which constitutes a promising advantage for this new class of antithrombotic agents.


Subject(s)
Fibrinolytic Agents/chemical synthesis , Platelet Aggregation Inhibitors/chemical synthesis , Receptor, PAR-1/antagonists & inhibitors , Animals , Drug Discovery , Drug-Related Side Effects and Adverse Reactions , Fibrinolytic Agents/administration & dosage , Humans , Piperazines/pharmacology , Platelet Aggregation Inhibitors/administration & dosage , Platelet Aggregation Inhibitors/pharmacology , Pyridines/pharmacology , Rats , Structure-Activity Relationship
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