Novel 2-aminobenzamides as potential orally active antithrombotic agents.

ACS Med Chem Lett

Pharmacy Department, Faculty of Technology & Engineering, Kalabhavan, The M. S. University of Baroda, Vadodara, 390001 Gujarat, India.

Published: January 2013

In an effort to develop potent antithrombotic agents, a series of novel 2-aminobenzamide derivatives were synthesized and screened for their in vivo antithrombotic activity. Among the 23 compounds tested, compound (8g) showed the most promising antithrombotic activity, which was comparable with clinically used aspirin or warfarin, but at variance with these standard drugs, 8g did not exhibit the increased bleeding time, suggesting its potential as a novel antithrombotic agent.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027566PMC
http://dx.doi.org/10.1021/ml300217fDOI Listing

Publication Analysis

Top Keywords

antithrombotic agents
8
antithrombotic activity
8
antithrombotic
5
novel 2-aminobenzamides
4
2-aminobenzamides potential
4
potential orally
4
orally active
4
active antithrombotic
4
agents effort
4
effort develop
4

Similar Publications

A Clinical Practice-Based Comparison of Conventional and Individualized Dosing Strategies for Therapeutic Enoxaparin.

Pharmacol Res Perspect

February 2025

Department of Internal Medicine, Royal Adelaide Hospital, Central Adelaide Local Health Network, Adelaide, South Australia, Australia.

To understand differences in anti-factor-Xa levels produced by two different dosing strategies (conventional and individualized) for therapeutic enoxaparin in a cohort of hospital inpatients. A multicenter, retrospective cohort study over a two- and a half-year period for inpatients with stable renal function and on therapeutic enoxaparin. Anti-factor-Xa levels were taken 3-5 h after enoxaparin administration and a minimum of 48 h of dosing.

View Article and Find Full Text PDF

Improvement in XIa Selectivity of Snake Venom Peptide Analogue BF9-N17K Using P2' Amino Acid Replacements.

Toxins (Basel)

January 2025

Institute of Biomedicine, Hubei Key Laboratory of Embryonic Stem Cell Research, College of Basic Medicine, Hubei University of Medicine, Shiyan 442000, China.

Coagulation factor XIa is a new serine-protease family drug target for next-generation anticoagulants. With the snake venom Kunitz-type peptide BF9 as the scaffold, we obtained a highly active XIa inhibitor BF9-N17K in our previous work, but it also inhibited the hemostatic target plasmin. Here, in order to enhance the selectivity of BF9-N17K toward XIa, four mutants, BF9-N17K-L19A, BF9-N17K-L19S, BF9-N17K-L19D, and BF9-N17K-L19K, were further designed using the P2' amino acid classification scanning strategy.

View Article and Find Full Text PDF

Acute massive pulmonary thromboembolism (PTE) is a potentially life-threatening condition requiring urgent management to decrease mortality. However, in the peripheral setting, managing the emergency can be challenging. We report a case of massive PTE presenting with cardiopulmonary arrest, successfully managed with advanced cardiac life support, early initiation of anticoagulants (heparin), and thrombolytics.

View Article and Find Full Text PDF

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.

View Article and Find Full Text PDF

Diabetes mellitus (DM) is a global health concern with a rising incidence, particularly in aging populations and those with a genetic predisposition. Over time, DM contributes to various complications, including nephropathy, retinopathy, peripheral arterial disease (PAD), and neuropathy. Among these, diabetic neuropathy and PAD stand out due to their high prevalence and significant impact on patients' quality of life.

View Article and Find Full Text PDF

Want 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!