Tetrazoles via multicomponent reactions

CG Neochoritis, T Zhao, A Domling - Chemical reviews, 2019 - ACS Publications
Tetrazole derivatives are a prime class of heterocycles, very important to medicinal
chemistry and drug design due to not only their bioisosterism to carboxylic acid and amide …

Direct thrombin inhibitors for anticoagulation

EA Nutescu, AK Wittkowsky - Annals of Pharmacotherapy, 2004 - journals.sagepub.com
OBJECTIVE: To review the progress in developing direct thrombin inhibitors (DTIs) for
anticoagulation within the context of existing anticoagulation therapies. DATA SOURCES …

Quantification of cation–π interactions in protein–ligand complexes: crystal‐structure analysis of factor Xa bound to a quaternary ammonium ion ligand

K Schärer, M Morgenthaler, R Paulini… - Angewandte Chemie …, 2005 - Wiley Online Library
The activities of inhibitors (Æ)-1 and (Æ)-2 were tested, as previously described,[7] towards
thrombin, the digestive enzyme trypsin, and two other serine proteases from the blood …

Bifunctional building blocks in the Ugi-azide condensation reaction: a general strategy toward exploration of new molecular diversity

S Gunawan, C Hulme - Organic & biomolecular chemistry, 2013 - pubs.rsc.org
1, 5-Disubstituted tetrazoles are an important drug-like scaffold known for their ability to
mimic the cis-amide bond conformation. The scaffold is readily accessible via substitution of …

Developments in factor Xa inhibitors for the treatment of thromboembolic disorders

YK Lee, MR Player - Medicinal Research Reviews, 2011 - Wiley Online Library
Thromboembolic diseases are the leading causes of morbidity and mortality in the
developed world. Anticoagulants provide effective treatment for venous or arterial …

New antithrombotic drugs on the horizon

J Ruef, HA Katus - Expert Opinion on Investigational Drugs, 2003 - Taylor & Francis
Venous and arterial thromboembolism are a major cause for morbidity and mortality. The list
of established drugs for the prevention of thrombus formation and embolisation includes …

[PDF][PDF] Novel heparan sulfate mimetic compounds as antitumor agents

K Ishida, MK Wierzba, T Teruya, S Simizu, H Osada - Chemistry & biology, 2004 - cell.com
Heparan sulfate glycosaminoglycans (HSGAGs) are involved in tumor cell growth, adhesion,
invasion, and migration, due to their interactions with various proteins. In this study, novel …

Virtual screening with flexible docking and COMBINE-based models. Application to a series of factor Xa inhibitors

M Murcia, AR Ortiz - Journal of medicinal chemistry, 2004 - ACS Publications
A two-step, fully automatic virtual screening procedure consisting of flexible docking
followed by activity prediction by COMparative BINding Energy (COMBINE) analysis is …

Synthesis of aminomethylated 4-fluoropiperidines and 3-fluoropyrrolidines

G Verniest, K Piron, E Van Hende… - Organic & …, 2010 - pubs.rsc.org
A short and efficient synthesis of 4-aminomethyl-4-fluoropiperidines and 3-aminomethyl-3-
fluoropyrrolidines is described. These fluorinated azaheterocycles are of specific interest as …

Design, synthesis, and biological activity of non-amidine factor Xa inhibitors containing pyridine N-oxide and 2-carbamoylthiazole units

N Haginoya, S Kobayashi, S Komoriya… - Bioorganic & medicinal …, 2004 - Elsevier
Based on the both of results for X-ray studies of tetrahydrothiazolopyridine derivative 1c and
FXV673, we synthesized a series of thiazol-5-ylpyridine derivatives containing pyridine N …