Factor Xa inhibitors: next-generation antithrombotic agents

DJP Pinto, JM Smallheer, DL Cheney… - Journal of medicinal …, 2010 - ACS Publications
Thrombosis is the underlying cause of a host of common, debilitating, and often fatal
cardiovascular disorders. Formation of thrombi in the arterial circulation can lead to acute …

Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines?

A Straub, S Roehrig, A Hillisch - … Chemie International Edition, 2011 - Wiley Online Library
To prevent thromboses after surgery, patients have until now had to inject themselves daily
with heparin. For stroke prophylaxis in atrial fibrillation, patients take vitamin K antagonists of …

CSAR benchmark exercise of 2010: combined evaluation across all submitted scoring functions

RD Smith, JB Dunbar Jr, PMU Ung… - Journal of chemical …, 2011 - ACS Publications
As part of the Community Structure-Activity Resource (CSAR) center, a set of 343 high-
quality, protein–ligand crystal structures were assembled with experimentally determined K …

Efficient Suzuki−Miyaura Coupling of (Hetero)aryl Chlorides with Thiophene- and Furanboronic Acids in Aqueous n-Butanol

CA Fleckenstein, H Plenio - The Journal of organic chemistry, 2008 - ACS Publications
An efficient Suzuki cross-coupling protocol enables the reaction of N-hetero and normal aryl
chlorides with thiophene-and furanboronic acids. Coupling is effected in aqueous n-butanol …

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N, N-dimethylcarbamimidoyl) benzamido)-5-methoxybenzamide, a highly potent, selective, and …

P Zhang, W Huang, L Wang, L Bao, ZJ Jia… - Bioorganic & medicinal …, 2009 - Elsevier
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were
performed by modifying each of the three phenyl rings. A class of highly potent, selective …

Highly efficient Suzuki–Miyaura coupling of heterocyclic substrates through rational reaction design

CA Fleckenstein, H Plenio - Chemistry–A European Journal, 2008 - Wiley Online Library
Abstract A dicyclohexyl (2‐sulfo‐9‐(3‐(4‐sulfophenyl) propyl)‐9H‐fluoren‐9‐yl)
phosphonium salt was synthesized in 64% overall yield in three steps from simple …

Discovery and development of Factor Xa inhibitors (2015–2022)

W Zheng, X Dai, B Xu, W Tian, J Shi - Frontiers in Pharmacology, 2023 - frontiersin.org
As a pathological coagulation process, thrombus can lead to many serious diseases,
including ischemic stroke, acute myocardial infarction (AMI), acute coronary syndrome …

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 …

Mechanistic QSAR analysis to predict the binding affinity of diverse heterocycles as selective cannabinoid 2 receptor inhibitor

RD Jawarkar, MEA Zaki, SA Al-Hussain… - Journal of Taibah …, 2023 - Taylor & Francis
CB2R are fascinating targets for neuropathic pain and mood disorders because of their
improved biological characteristics. Experimental data on 1296 cannabinoid-2 receptor …

Anthranilic acid-based diamides derivatives incorporating aryl-isoxazoline pharmacophore as potential anticancer agents: Design, synthesis and biological evaluation

L Shi, R Hu, Y Wei, Y Liang, Z Yang, S Ke - European journal of medicinal …, 2012 - Elsevier
A series of novel anthranilic diamides derivatives containing aryl-isoxazoline moiety were
designed and synthesized as a part of our ongoing search for potential anticancer agents …