Deuterated Clopidogrel Analogues as a New Generation of Antiplatelet Agents was written by Zhu, Yaoqiu;Zhou, Jiang;Jiao, Bo. And the article was included in ACS Medicinal Chemistry Letters in 2013.Electric Literature of C7H8O2S This article mentions the following:
Clopidogrel (CPG) is an antithrombotic prodrug that needs hepatic cytochrome P 450 (CYP) enzymes for its bioactivation. The clin. effects of CPG have been associated with high intersubject variability and a certain level of resistance. Recently, comprehensive biotransformation studies of CPG support that the observed clin. uncertainty stems from the low bioactivation efficiency, which is attributed to extensive attritional metabolism (e.g., hydrolysis of the Me ester functionality and oxidation of the piperidine moiety). With the goal of potentiating the desired thiophene 2-oxidation through minimal structural modification, we have adopted the strategy of targeted metabolism shift and have designed and synthesized deuterated piperidine analogs of CPG. In vitro studies showed that the prodrug activation percentages have been significantly increased for the deuterated analogs as a result of stability enhancement of the piperidine moiety. In a pharmacol. study with a rat model, oral administration of the deuterated analogs also demonstrated higher inhibitory activity than that of CPG against ADP (ADP) induced platelet aggregation. These deuterated analogs represent a new generation of antiplatelet agents with the potential to overcome the major clin. drawbacks of CPG. In the experiment, the researchers used many compounds, for example, Methyl 2-thienylacetate (cas: 19432-68-9Electric Literature of C7H8O2S).
Methyl 2-thienylacetate (cas: 19432-68-9) belongs to esters. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 绾?valerolactone.Electric Literature of C7H8O2S
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics