In our continuing effort to discover compound which inhibit collagen-induced platelet aggregation, we have screened compounds in a mouse pulmonary thromboembolism screen. Methyl 4,5-bis(4-methoxyphenyl)-2-thiazoleacetate (3) was very active in the above screen. However, 3 was active for less than 5 min when given orally to guinea pigs. As a result, our synthetic goal was to prepare 2-substituted thiazoles with a much longer duration of activity. This paper describes the preparation of a number 4,5-bis(aryl)-2-substituted-thiazoles and their in vitro and ex vivo activity against collagen-induced platelet aggregation. It was determined that 4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)thiazole (16) is the most promising compound.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00144a026 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Platelet Function Assay Using Dielectric Blood Coagulometry.
Anal Chem
January 2025
Department of Anesthesiology, Tokyo Medical and Dental University, Graduate School of Medical and Dental Sciences, 1-5-45 Yushima, Bunkyo-ku 113-8510, Tokyo, Japan.
The hemostatic function of platelets is complementary to blood coagulation. However, traditional platelet function tests have primarily focused on measuring platelet aggregation, reducing their clinical effectiveness for antiplatelet drug monitoring. To address this limitation, we propose a new test principle that evaluates platelet function and the effects of antiplatelet drugs through blood coagulation reactions.
View Article and Find Full Text PDFEffect of antiplatelet and anticoagulant medications on implant survival: a long-term retrospective cohort study.
Oral Maxillofac Surg
January 2025
Department of Developmental and Surgical Sciences, Division of Periodontology, School of Dentistry, University of Minnesota, 515 Delaware Street SE, Minneapolis, MN, 55455, USA.
Purpose: This large-scale retrospective study aimed to examine the long-term effect of antiplatelet and anticoagulant medications intake on dental implant treatment outcome.
Materials And Methods: This study retrospectively examined data from patients who underwent dental implant procedures at several university dental clinics within the BigMouth network between 2011 and 2022. Patients' characteristics including age, gender, ethnicity, race, tobacco use, systemic medical conditions and intake of antiplatelets and anticoagulants were analyzed.
Cessation vs. no cessation of acetylsalicylic acid preoperatively in laparoscopic totally extraperitoneal inguinal hernia repair (CAPTAIN): interim report from a multicentre, single-blind, randomised controlled trial.
Hernia
January 2025
Department of Minimally Invasive Surgery, National University Hospital, Bukit Timah, Singapore.
Background: Given the increasing prevalence of antiplatelet agent use and the lack of high-quality evidence, the CAPTAIN trial aimed to investigate the safety and provide recommendations on continuing acetylsalicylic acid perioperatively in patients undergoing elective laparoscopic totally extraperitoneal inguinal hernia repair (LIHR).
Methods: The CAPTAIN trial was a multicentre, surgeon blind, randomized controlled trial conducted from April 2016 to April 2023. Patients undergoing LIHR were eligible for inclusion.
Changes in platelet maturity and reactivity following acute ST-segment elevation myocardial infarction.
Res Pract Thromb Haemost
January 2025
Department of Cardiology, Aarhus University Hospital, Aarhus, Denmark.
Background: Reduced effect of antiplatelet therapy has been reported in patients with ST-segment elevation myocardial infarction (STEMI). This could partly be explained by an increase of highly reactive immature platelets.
Objectives: To investigate changes in platelet maturity and reactivity after acute STEMI.
[Determination of three metabolites of thromboxane A and 8-iso-prostaglandin F in urine by ultra performance liquid chromatography-tandem mass spectrometry].
Se Pu
February 2025
Shanghai-MOST Key Laboratory of Health and Disease Genomics, NHC Key Lab of Reproduction Regulation, Shanghai Institute for Biomedical and Pharmaceutical Technologies, Shanghai 200237, China.
Thromboxane A (TXA), a prothrombotic factor that induces platelet aggregation and thrombosis, acts as a vasoconstrictor by activating TXA receptors (TP receptors). TXA is extremely unstable and metabolizes into three major metabolites: 2,3-dinor thromboxane B (2,3-dinor-TXB), 11-dehydro TXB(11-dh-TXB), and 11-dehydro-2,3-dinor TXB(11-dh-2,3-dinor-TXB). 8-Iso-prostaglandin F(8-iso-PGF), a prostaglandin-like compound widely considered the best biomarker of oxidative stress, can also activate TP receptors.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!