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C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 1998 Jul 07; Vol. 8 (13), pp. 1719-24. - Publication Year :
- 1998
-
Abstract
- 1 (L-374,087) is a potent, selective, efficacious, and orally bioavailable thrombin inhibitor that contains a core 3-amino-2-pyridinone moiety. Replacement of the C6 pyridinone methyl group of 1 by a propyl group gave 5 (L-375,052), which retained all the excellent properties of 1, and also yielded higher plasma levels after oral dosing in dogs and rats.
- Subjects :
- Administration, Oral
Animals
Antithrombins administration & dosage
Biological Availability
Dogs
Pyridines chemistry
Pyridines pharmacokinetics
Pyridines pharmacology
Pyridones pharmacology
Rats
Sulfanilamides chemistry
Sulfanilamides pharmacokinetics
Sulfanilamides pharmacology
Sulfonamides pharmacology
Antithrombins chemistry
Antithrombins pharmacokinetics
Pyridones chemistry
Pyridones pharmacokinetics
Sulfonamides chemistry
Sulfonamides pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 8
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 9873422
- Full Text :
- https://doi.org/10.1016/s0960-894x(98)00297-2