Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors

DO Arnaiz, A Liang, L Trinh, M Whitlow… - Bioorganic & Medicinal …, 2000 - Elsevier
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors -
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Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with biaryl P4 motifs

RJ Young, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2008 - Elsevier
Structure and property based drug design was exploited in the synthesis of
sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups …

Structure-and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs

RJ Young, M Campbell, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2006 - Elsevier
Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-
ylsulfonyl) aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an …

Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors

S Robert, C Bertolla, B Masereel… - Journal of medicinal …, 2008 - ACS Publications
Recently, FXIIa was highlighted as an original attractive target for the development of new
anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe …

Synthesis, Docking, and In Vitro Anticoagulant Activity Assay of Hybrid Derivatives of Pyrrolo[3,2,1-ij]Quinolin-2(1H)-one as New Inhibitors of Factor Xa and Factor …

N Novichikhina, I Ilin, A Tashchilova, A Sulimov… - Molecules, 2020 - mdpi.com
Coagulation factor Xa and factor XIa are proven to be convenient and crucial protein targets
for treatment for thrombotic disorders and thereby their inhibitors can serve as effective …

New Hybrid Tetrahydropyrrolo[3,2,1-ij]quinolin-1-ylidene-2-thioxothiazolidin-4-ones as New Inhibitors of Factor Xa and Factor XIa: Design, Synthesis, and In Silico …

NP Novichikhina, AS Shestakov, SM Medvedeva… - Molecules, 2023 - mdpi.com
Despite extensive research in the field of thrombotic diseases, the prevention of blood clots
remains an important area of study. Therefore, the development of new anticoagulant drugs …

Orally active factor Xa inhibitors: 4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine derivatives

N Haginoya, S Kobayashi, S Komoriya… - Bioorganic & medicinal …, 2004 - Elsevier
In our investigation of factor Xa inhibitors, a series of 1-(6-chloronaphthalen-2-yl) sulfonyl-4-
(4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine-2-carbonyl) piperazines 3a–i were synthesized …

Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors

T Ishihara, N Seki, F Hirayama, M Orita… - Bioorganic & medicinal …, 2007 - Elsevier
We describe here our investigation of a new series of orally active fXa inhibitors based on a
prodrug strategy. Solid-phase parallel synthesis identified a unique series of fXa inhibitors …

(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one:  Identification of a Highly Active Inhibitor of Blood Coagulation Factor Xa

KJ Shaw, WJ Guilford, JL Dallas… - Journal of medicinal …, 1998 - ACS Publications
Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in the blood
coagulation cascade. It holds a central position that links the intrinsic and extrinsic pathways …

Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors

ML Quan, JR Pruitt, CD Ellis, AY Liauw… - Bioorganic & Medicinal …, 1997 - Elsevier
Factor Xa is an important serine protease in the blood coagulation cascade. It generates
thrombin and holds the central position that links the intrinsic and extrinsic activation …