ArticleChemMedChem2021
Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors.
Article in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 22 citations in OpenAlex.
- Development of an Interpretable QSAR Model for Predicting Coagulation Factor XIIa Inhibitors Using Ensemble Machine Learning.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Evaluation of Machine Learning Models for Condition Optimization in Diverse Amide Coupling Reactions.ACS omega · 2026Article
- Recent advances in non-conventional synthesis of N-heterocyclic compounds: emerging strategies and biological perspectives.RSC advances · 2025Review
- Pyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties.ACS pharmacology & translational science · 2025Article
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- Biological evaluation of semi-synthetic isoindolinone isomers produced byFrontiers in fungal biology · 2024Article
- Microwave-Assisted Synthesis, Structure, and Preliminary Biological Evaluation of Novel 6-Methoxy-5,6-dihydro-5-azapurines.ACS omega · 2023Article
- Semisynthetic Approach toward Biologically Active Derivatives of Phenylspirodrimanes fromACS omega · 2022Article
- Amide-functionalized 1,2,4-Triazol-5-amines as Covalent Inhibitors of Blood Coagulation Factor XIIa and Thrombin.ACS pharmacology & translational science · 2022Article
- Pyrazole-Based Thrombin Inhibitors with a Serine-Trapping Mechanism of Action: Synthesis and Biological Activity.Pharmaceuticals (Basel, Switzerland) · 2022Article
- New Blood Coagulation Factor XIIa Inhibitors: Molecular Modeling, Synthesis, and Experimental Confirmation.Molecules (Basel, Switzerland) · 2022Article
- Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors.ChemMedChem · 2021Article
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9 authors at 1 institution in 1 country.
Funding
Abstract
Herein we report a microscale parallel synthetic approach allowing for rapid access to libraries of N-acylated aminotriazoles and screening of their inhibitory activity against factor XIIa (FXIIa) and thrombin, which are targets for antithrombotic drugs. This approach, in combination with post-screening structure optimization, yielded a potent 7 nM inhibitor of FXIIa and a 25 nM thrombin inhibitor; both compounds showed no inhibition of the other tested serine proteases. Selected N-acylated aminotriazoles exhibited anticoagulant properties in vitro influencing the intrinsic blood coagulation pathway, but not extrinsic coagulation. Mechanistic studies of FXIIa inhibition suggested that synthesized N-acylated aminotriazoles are covalent inhibitors of FXIIa. These synthesized compounds may serve as a promising starting point for the development of novel antithrombotic drugs.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.