An Overview of Thrombin Inhibitors in the Perspective of Structure-activity Relationships

被引：3

作者：

Wang, Jiangming ^{[1
]}

Sun, Xiaojing ^{[1
]}

Li, Na ^{[1
]}

Sheng, Ruilong ^{[2
]}

Guo, Ruihua ^{[1
,3
,4
]}

机构：

[1] Shanghai Ocean Univ, Coll Food Sci & Technol, Shanghai 201306, Peoples R China

[2] Univ Madeira, CQM Cent Quim Madeira, Campus Penteada, P-9000390 Funchal, Portugal

[3] Shanghai Engn Res Ctr Aquat Prod Proc & Preservat, Shanghai 201306, Peoples R China

[4] Minist Agr, Lab Qual & Safety Risk Assessment Aquat Prod Stora, Shanghai 201306, Peoples R China

来源：

CURRENT MEDICINAL CHEMISTRY | 2023年 / 30卷 / 25期

基金：

中国国家自然科学基金;

关键词：

Antithrombotic; thrombin inhibitor; structure-activity relationship; pharmacokinetics; PROTEASE-ACTIVATED RECEPTORS; DESIGNING ALLOSTERIC REGULATORS; OPTIMIZING PLATELET INHIBITION; ORALLY BIOAVAILABLE SERIES; FACTOR XA INHIBITORS; BIOLOGICAL EVALUATION; ANTITHROMBOTIC COMPOUNDS; IN-VITRO; PART; SCUTELLAREIN DERIVATIVES;

D O I：

10.2174/0929867329666220906105200

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Thrombosis is one of the most important pathogenic factors related to cardiovascular diseases. Presently, thrombin inhibitors have gradually gained prominence in clinical practice due to their unique potential, such as dabigatran. Nevertheless, the risk of bleeding is not completely eliminated, and the threats of gastrointestinal bleeding are even increased in some cases. Therefore, developing new oral thrombin inhibitors with low side effects is urgent. In this paper, we summarized recent advances in the newly synthesized and isolated thrombin inhibitors from 2000 to 2019 and their structure-activity relationships (SARs) along with structure-dependent pharmacokinetic parameters, guiding the next generation of oral thrombin inhibitors.

引用

页码：2864 / 2930

页数：67

共 181 条

[1] Discovery of AZD8165-a clinical candidate from a novel series of neutral thrombin inhibitors [J].

Abrahamsson, K. ;

Andersson, P. ;

Bergman, J. ;

Bredberg, U. ;

Branalt, J. ;

Egnell, A. -C. ;

Eriksson, U. ;

Gustafsson, D. ;

Hoffman, K. -J. ;

Nielsen, S. ;

Nilsson, I. ;

Pehrsson, S. ;

Polla, M. O. ;

Skjaeret, T. ;

Strimfors, M. ;

Wern, C. ;

Olwegard-Halvarsson, M. ;

Ortengren, Y. .

MEDCHEMCOMM, 2016, 7 (02) :272-281

[2] A small group of sulfated benzofurans induces steady-state submaximal inhibition of thrombin [J].

Afosah, Daniel K. ;

Verespy, Stephen, III ;

Al-Horani, Rami A. ;

Boothello, Rio S. ;

Karuturi, Rajesh ;

Desai, Umesh R. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (06) :1101-1105

[3] Recent advances in the discovery and development of factor XI/XIa inhibitors [J].

Al-Horani, Rami A. ;

Afosah, Daniel K. .

MEDICINAL RESEARCH REVIEWS, 2018, 38 (06) :1974-2023

[4] Factor XIa inhibitors: A review of the patent literature [J].

Al-Horani, Rami A. ;

Desai, Umesh R. .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2016, 26 (03) :323-345

[5] Effects of warfarin on biological processes other than haemostasis: A review [J].

Aleksandrov, Aleksandra Popov ;

Mirkov, Ivana ;

Ninkov, Marina ;

Mileusnic, Dina ;

Demenesku, Jelena ;

Subota, Vesna ;

Kataranovski, Dragan ;

Kataranovski, Milena .

FOOD AND CHEMICAL TOXICOLOGY, 2018, 113 :19-32

[6] Thrombin Inhibitors from the Freshwater Cyanobacterium Anabaena compacta [J].

Anas, Andrea Roxanne J. ;

Kisugi, Takaya ;

Umezawa, Taiki ;

Matsuda, Fuyuhiko ;

Campitelli, Marc R. ;

Quinn, Ronald J. ;

Okino, Tatsufumi .

JOURNAL OF NATURAL PRODUCTS, 2012, 75 (09) :1546-1552

[7] Toward a novel class of antithrombotic compounds with dual function.: Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities [J].

Anderluh, PS ;

Anderluh, M ;

Ilas, J ;

Mravljak, J ;

Dolenc, MS ;

Stegnar, M ;

Kikelj, D .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (09) :3110-3113

[8] Optimizing Platelet Inhibition in Clopidogrel Poor Metabolizers Therapeutic Options and Practical Considerations [J].

Angiolillo, Dominick J. ;

Ueno, Masafumi .

JACC-CARDIOVASCULAR INTERVENTIONS, 2011, 4 (04) :411-414

[9] Platelet thrombin receptor antagonism and atherothrombosis [J].

Angiolillo, Dominick J. ;

Capodanno, Davide ;

Goto, Shinya .

EUROPEAN HEART JOURNAL, 2010, 31 (01) :17-25

[10] Protease-activated Receptors and Myocardial Infarction [J].

Antoniak, Silvio ;

Pawlinski, Rafal ;

Mackman, Nigel .

IUBMB LIFE, 2011, 63 (06) :383-389

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