Parallel synthesis and structure–activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors

Parallel synthesis and structure–activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors

Parallel synthesis and iterative optimization led to the discovery of a series of inhibitors having excellent in vitro and promising in vivo properties. Parallel synthesis and iterative optimization led to the discovery of a series of potent and specific factor Xa inhibitors demonstrating excellent...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 14; no. 15; pp. 4045 - 4050
Main Authors: Bauer, Shawn M, Goldman, Erick A, Huang, Wenrong, Su, Ting, Wang, Lingyan, Woolfrey, John, Wu, Yanhong, Zuckett, Jingmei F, Arfsten, Ann, Huang, Brian, Kothule, Jaya, Lin, Joyce, May, Bridget, Sinha, Uma, Wong, Paul W, Hutchaleelaha, Athiwat, Scarborough, Robert M, Zhu, Bing-Yan
Format: Journal Article
Language:English
Published: Oxford Elsevier Ltd 02-08-2004
Elsevier
Subjects:
Amino acid
Antithrombin III - chemical synthesis
Antithrombin III - pharmacology
Aspartic acid
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Factor Xa
Factor Xa Inhibitors
Humans
Medical sciences
Miscellaneous
Molecular Conformation
Molecular Structure
Pharmacology. Drug treatments
SAR
Structure-Activity Relationship
Factor Xa
Aspartic acid
Amino acid
SAR
Serine endopeptidases
Enzyme
Combinatorial chemistry
Enzyme inhibitor
Coagulation Factor Xa
Anticoagulant
Selectivity
In vitro
Biological activity
Peptidases
Structure activity relation
Hydrolases
Pharmacokinetics
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Summary:Parallel synthesis and iterative optimization led to the discovery of a series of inhibitors having excellent in vitro and promising in vivo properties. Parallel synthesis and iterative optimization led to the discovery of a series of potent and specific factor Xa inhibitors demonstrating excellent in vitro activity with promising pharmacokinetics.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.05.033