Design, Synthesis and Biological Actmty of Novel Rigid Amidino-Phenylalanine Derivatives as Inhibitors of Thrombin

Helmut Mack Main Laboratoty, Pharmaceuticals Research, BASF AG, Ludwigshafen, D-67056, Germany

Thomas Pfeiffer Main Laboratoty, Pharmaceuticals Research, BASF AG, Ludwigshafen, D-67056, Germany

Wilfried Hornberger Knoll, Department of Angiology, BASF AG, Ludwigshafen, D-67056, Germany

Hans-Joachim Böhm Main Laboratoty, Pharmaceuticals Research, BASF AG, Ludwigshafen, D-67056, Germany

Hans Wolfgang Höffken Main Laboratoty, Pharmaceuticals Research, BASF AG, Ludwigshafen, D-67056, Germany

Abstract

(3S)-(Naphthalene-2-sulfonylamino)-1-[2R-(4-amidinophenyl)-1-piperidinocarbonylethyl]-2-pyrroli-dinone (1a) is a potent inhibitor of thrombin with an IC₅₀ value by 112 times lower than that of NAPAF’ (racemate). The selectivity versus trypsin can be improved by incorporation of substituents on the naphthyl ring. The mode of binding of the compound was determined by X-ray crystallography.

Key Words: :

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Design, Synthesis and Biological Actmty of Novel Rigid Amidino-Phenylalanine Derivatives as Inhibitors of Thrombin

Information for

Open access

Opportunities

Help and information

Design, Synthesis and Biological Actmty of Novel Rigid Amidino-Phenylalanine Derivatives as Inhibitors of Thrombin

Abstract

Reprints and Corporate Permissions

Academic Permissions

Related research

To cite this article:

Download citation

Information for

Open access

Opportunities

Help and information

Keep up to date

Your download is now in progress and you may close this window

Login or register to access this feature