Page 111 - GTM-4-2

Global Translational Medicine

BRIEF REPORT
Platelet aggregation inhibition by fluorophenyl-

substituted 2-isoxazoline-5-carboxylic acids and
their derivatives

Mikalai M. Kauhanka* , Marharita E. Parkhach , Svetlana N. Borisevich ,
Stanislava V. Glinnik , and Elena N. Haluk
Department of General Chemistry, Career Guidance and Pre-University Training Faculty, Belarusian
State Medical University, Minsk, Belarus
(This article belongs to the Special Issue: Special Issue of Global Translational Medicine in the
Fourth RCCCDT-2024)

Abstract
Platelets perform many important bodily functions, with their primary task being the
prevention of bleeding by facilitating hemostasis. While platelets protect the body
from blood loss, they also contribute to the development of serious diseases, such as
atherosclerosis and its complications. Understanding the dual role of platelets is crucial
for developing new treatments aimed at reducing thrombotic risk while improving
the prognosis for patients with cardiovascular diseases. Specifically, elucidating
*Corresponding author:
Mikalai M. Kauhanka the mechanisms underlying platelet activation may facilitate the development of
(mikalai44@tut.by) selective agents that inhibit pathological platelet activity without compromising
Citation: Kauhanka MM, their protective function. In this context, the present study evaluated the antiplatelet
Parkhach ME, Borisevich SN, activity of newly synthesized fluorophenyl-substituted 2-isoxazoline-5-carboxylic
Glinnik SV, Haluk EN. Platelet acids and their derivatives. Results showed that all compounds demonstrated the
aggregation inhibition by
fluorophenyl-substituted ability to suppress platelet aggregation. Increasing the concentration of the active
2-isoxazoline-5-carboxylic acids and substance from 1 to 25 mmol/L enhanced the inhibitory effect of the compounds.
their derivatives. Global Transl Med. Methyl esters, compared to derivatives with a free carboxyl group, exhibited a
2025;4(2):103-108.
doi: 10.36922/gtm.8147 stronger ability to suppress the activation of platelet receptors glycoprotein (GP)
IIa/IIIb, thereby inhibiting their binding to fibrinogen and subsequent aggregation.
Received: December 23, 2024 The half-maximal inhibitory concentration values for two of the studied compounds
1st revised: February 24, 2025 were 7.5 mmol/L (methyl ester of 3- -fluorophenyl]-2-isoxazoline carboxylic acid)
[3
[2
2nd revised: February 26, 2025 and 12.5 mmol/L (methyl ester of 3- -fluorophenyl]-2-isoxazoline carboxylic acid),
respectively. In conclusion, the findings of this study indicate that 3-aryl-2-isoxazoline-
Accepted: March 20, 2025 5-carboxylic acids and their methyl esters, containing a single fluorine atom in the aryl
Published online: April 4, 2025 group, effectively suppress the activation of platelet receptors GPIIa/IIIb.
Copyright: © 2025 Author(s).
This is an Open-Access article
distributed under the terms of the Keywords: Antiplatelet agent; Heterocycle; 2-isoxazoline; Platelet; Flow cytometry
Creative Commons Attribution
License, permitting distribution,
and reproduction in any medium,
provided the original work is
properly cited. 1. Introduction
Publisher’s Note: AccScience Platelets, or thrombocytes, are essential components of the hemostatic system, playing a
Publishing remains neutral with key role in preventing blood loss during trauma. However, their function extends beyond
regard to jurisdictional claims in
published maps and institutional merely protecting the body against bleeding. Platelets are also involved in pathological
affiliations. mechanisms, leading to thrombus formation, which can cause acute vascular diseases,

Volume 4 Issue 2 (2025) 103 doi: 10.36922/gtm.8147