ArticleACS medicinal chemistry letters2013
Deuterated clopidogrel analogues as a new generation of antiplatelet agents.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 76 citations in OpenAlex.
- Total Syntheses of Deuterated Drugs: A Comprehensive Review.Topics in current chemistry (Cham) · 2025Review
- Designing chemical systems for precision deuteration of medicinal building blocks.Nature communications · 2024Article
- Deuterium in drug discovery: progress, opportunities and challenges.Nature reviews. Drug discovery · 2023Review
- The impact of H/D exchange on the thermal and structural properties as well as high-pressure relaxation dynamics of melatonin.Scientific reports · 2022Article
- Rational deuteration of dronedarone attenuates its toxicity in human hepatic HepG2 cells.Toxicology research · 2022Article
- Titanocene(III)-Catalyzed Precision Deuteration of Epoxides.Angewandte Chemie (International ed. in English) · 2022Article
- Rhodium(iii) catalyzed olefination and deuteration of tetrahydrocarbazole.RSC advances · 2021Article
- Silver-catalyzed regioselective deuteration of (hetero)arenes and α-deuteration of 2-alkyl azaarenes.RSC advances · 2020Article
- Bioinspired design of a robustScience advances · 2020Article
- Formyl-selective deuteration of aldehydes with DChemical science · 2019Article
- Effect of N-methyl deuteration on metabolism and pharmacokinetics of enzalutamide.Drug design, development and therapy · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Clopidogrel (CPG) is an antithrombotic prodrug that needs hepatic cytochrome P450 (CYP) enzymes for its bioactivation. The clinical 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 clinical uncertainty stems from the low bioactivation efficiency, which is attributed to extensive attritional metabolism (e.g., hydrolysis of the methyl 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 analogues of CPG. In vitro studies showed that the prodrug activation percentages have been significantly increased for the deuterated analogues as a result of stability enhancement of the piperidine moiety. In a pharmacological study with a rat model, oral administration of the deuterated analogues also demonstrated higher inhibitory activity than that of CPG against adenosine diphosphate (ADP) induced platelet aggregation. These deuterated analogues represent a new generation of antiplatelet agents with the potential to overcome the major clinical drawbacks of CPG.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.