Contemporary developments in the discovery of selective factor Xa inhibitors: A review

NR Patel, DV Patel, PR Murumkar, MR Yadav - European journal of …, 2016 - Elsevier
Thrombosis is a leading cause of death in cardiovascular diseases such as myocardial
infarction (MI), unstable angina and acute coronary syndrome (ACS) in the industrialized …

Acceptance and kinetic resolution of α-methyl-substituted aldehydes by norcoclaurine synthases

R Roddan, G Gygli, A Sula, D Méndez-Sánchez… - ACS …, 2019 - ACS Publications
Norcoclaurine synthase (NCS) catalyzes a stereoselective Pictet–Spengler reaction to give
the key intermediate,(S)-norcoclaurine in benzylisoquinoline alkaloid biosynthesis. This …

Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors …

F Santana-Romo, CF Lagos, Y Duarte, F Castillo… - Molecules, 2020 - mdpi.com
The coagulation cascade is the process of the conversion of soluble fibrinogen to insoluble
fibrin that terminates in production of a clot. Factor Xa (FXa) is a serine protease involved in …

Sulfonated nonsaccharide heparin mimetics are potent and noncompetitive inhibitors of human neutrophil elastase

RA Al-Horani, KF Aliter, S Kar, M Mottamal - ACS omega, 2021 - ACS Publications
Human neutrophil elastase (HNE) is a serine protease that plays vital roles in inflammation,
innate immune response, and tissue remodeling processes. HNE has been actively pursued …

Review on Synthetic Approaches toward Rivaroxaban (Xarelto), an Anticoagulant Drug

DY Mladentsev, EN Kuznetsova… - … Process Research & …, 2022 - ACS Publications
Venous thromboembolism including deep vein thrombosis and pulmonary embolism is an
abundant and dangerous disease with significant relapse probability and mortality. In pursuit …

Lignosulfonic acid sodium is a noncompetitive inhibitor of human factor XIa

S Kar, P Bankston, DK Afosah, RA Al-Horani - Pharmaceuticals, 2021 - mdpi.com
The anticoagulant activity of lignosulfonic acid sodium (LSAS), a non-saccharide heparin
mimetic, was investigated in this study. LSAS is a relatively safe industrial byproduct with …

Design, synthesis and biological evaluation of novel 2, 3-dihydroquinazolin-4 (1H)-one derivatives as potential fXa inhibitors

J Xing, L Yang, Y Yang, L Zhao, Q Wei, J Zhang… - European Journal of …, 2017 - Elsevier
Coagulation factor Xa (fXa) is a particularly attractive target for the development of effective
and safe anticoagulants. In this study, novel 2, 3-dihydroquinazolin-4 (1 H)-one derivatives …

Discovery of glycyrrhetinic acid as an orally active, direct inhibitor of blood coagulation factor xa

L Jiang, Q Wang, S Shen, T Xiao, Y Li - Thrombosis research, 2014 - Elsevier
Abstract Introduction Factor Xa (FXa) plays an important role in blood coagulation. This
study investigated glycyrrhetinic acid, a small molecule derived from Chinese herbs, and …

[HTML][HTML] Plasmin regulation through allosteric, sulfated, small molecules

RA Al-Horani, R Karuturi, DT White, UR Desai - Molecules, 2015 - mdpi.com
Plasmin, a key serine protease, plays a major role in clot lysis and extracellular matrix
remodeling. Heparin, a natural polydisperse sulfated glycosaminoglycan, is known to …

[HTML][HTML] (1R, 3S)-THCCA-Asn: To show the discovery of selective inhibitor of thrombin by successfully combining virtual screening and biological assay

X Zhang, Y Yang, Y Wang, J Wu, Q Fang… - European Journal of …, 2022 - Elsevier
Thrombin is the most potent platelet aggregator. To discover the selective inhibitor of
thrombin that is important to curing platelet aggregation-related diseases, docking …