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Molecules
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Anticoagulant and Antithrombotic Therapy
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Anticoagulant and Antithrombotic Therapy

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 April 2024) | Viewed by 1168

Special Issue Editors

Prof. Dr. Cosimo D. Altomare

E-Mail Website
Guest Editor
Department of Pharmacy-Pharmaceutical Sciences, University of Bari, Bari, Italy
Interests: medicinal chemistry of medium-sized azaheterocyclic compounds; multitarget-directed ligands (LTDLs) for treating Alzheimer's disease and other neurodegeneration syndromes; new oral anticoagulants (NOACs); physicochemical parametrization in ADMET studies; molecular modeling, computational chemistry and three-dimensional quantitative structure-activity relationships (3D-QSARs)
Special Issues, Collections and Topics in MDPI journals
Dr. Modesto De Candia

E-Mail Website
Guest Editor
Department of Pharmacy-Pharmaceutical Sciences, University of Bari, Bari, Italy
Interests: medicinal chemistry of multitarget-directed ligands (LTDLs) targeted at neurodegeneration; design, synthesis and structure-activity relationships of new oral anticoagulants (NOACs) and antiplatelet agents; biophysical characterization of kinetics and thermodynamics of interaction with different protein targets, involved in diseases onset and drug distribution profile
Special Issues, Collections and Topics in MDPI journals
Dr. Rosa Purgatorio

E-Mail Website
Guest Editor
Department of Pharmacy-Pharmaceutical Sciences, University of Bari, Bari, Italy
Interests: design and synthesis of azaheterocycle small molecules as multitarget-directed ligands (MTDLs) for neurodegenerative diseases; synthesis of new inhibitors of blood coagulation factors; pharmaceutical analysis

Special Issue Information

Dear Colleagues,

It is our pleasure to announce the launch of a new Molecules Special Issue on “Anticoagulant and Antithrombotic Therapy”. Antiplatelet agents and anticoagulants represent a mainstay for the prevention and treatment of thrombosis-related diseases. However, despite the undoubted advances in antithrombotic therapy, bleeding still remains a major side effect. Understanding the mechanisms of hemostasis and thrombosis has revealed new targets for attenuating thrombosis with the potential for less bleeding.

The recently developed direct oral anticoagulants (DOACs), targeting coagulation cascade factors such as thrombin (dabigatran) or fXa (apixaban, edoxaban, and rivaroxaban), significantly expand the available warehouse of antithrombotic agents. The ultimate goal of anticoagulation therapy is to attenuate thrombosis without perturbing hemostasis, and DOACs come closer to this goal, without the elimination of bleeding risk. New targets (FXIIa and FXIa) or molecular strategies (allosteric inhibitors or modulators, antisense oligonucleotides, monoclonal antibodies, and aptamers) have evolved in the identification of new active compounds. This Special Issue will focus on the recent advances, current challenges, and future perspectives of antithrombotic agents.

Prof. Dr. Cosimo D. Altomare
Dr. Modesto De Candia
Dr. Rosa Purgatorio
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • thrombosis
  • coagulation cascade
  • platelet aggregation
  • anticoagulants
  • antiplatelet agents
  • antithrombotics
  • drug design
  • coagulative enzyme inhibitors
  • synthesis
  • molecular docking
  • structure–activity relationships
  • antisense oligonucleotides
  • monoclonal antibodies

Published Papers (1 paper)

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Research

18 pages, 2476 KiB  
Article
Design, Synthesis, and Evaluation of New Hybrid Derivatives of 5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-2(1H)-one as Potential Dual Inhibitors of Blood Coagulation Factors Xa and XIa
by Anna A. Skoptsova, Athina Geronikaki, Nadezhda P. Novichikhina, Alexey V. Sulimov, Ivan S. Ilin, Vladimir B. Sulimov, Georgii A. Bykov, Nadezhda A. Podoplelova, Oleg V. Pyankov and Khidmet S. Shikhaliev
Molecules 2024, 29(2), 373; https://doi.org/10.3390/molecules29020373 - 11 Jan 2024
Viewed by 770
Abstract
Cardiovascular diseases caused by blood coagulation system disorders are one of the leading causes of morbidity and mortality in the world. Research shows that blood clotting factors are involved in these thrombotic processes. Among them, factor Xa occupies a key position in the [...] Read more.
Cardiovascular diseases caused by blood coagulation system disorders are one of the leading causes of morbidity and mortality in the world. Research shows that blood clotting factors are involved in these thrombotic processes. Among them, factor Xa occupies a key position in the blood coagulation cascade. Another coagulation factor, XIa, is also a promising target because its inhibition can suppress thrombosis with a limited contribution to normal hemostasis. In this regard, the development of dual inhibitors as new generation anticoagulants is an urgent problem. Here we report the synthesis and evaluation of novel potential dual inhibitors of coagulation factors Xa and XIa. Based on the principles of molecular design, we selected a series of compounds that combine in their structure fragments of pyrrolo[3,2,1-ij]quinolin-2-one and thiazole, connected through a hydrazine linker. The production of new hybrid molecules was carried out using a two-stage method. The reaction of 5,6-dihydropyrrolo[3,2,1-ij]quinoline-1,2-diones with thiosemicarbazide gave the corresponding hydrazinocarbothioamides. The reaction of the latter with DMAD led to the target methyl 2-(4-oxo-2-(2-(2-oxo-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1(2H)-ylidene)hydrazineyl)thiazol-5(4H)-ylidene)acetates in high yields. In vitro testing of the synthesized molecules revealed that ten of them showed high inhibition values for both the coagulation factors Xa and XIa, and the IC50 value for some compounds was also assessed. The resulting structures were also tested for their ability to inhibit thrombin. Full article
(This article belongs to the Special Issue Anticoagulant and Antithrombotic Therapy)
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