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1mu8

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(New page: 200px<br /> <applet load="1mu8" size="450" color="white" frame="true" align="right" spinBox="true" caption="1mu8, resolution 2.0&Aring;" /> '''thrombin-hirugen_l-3...)
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Revision as of 16:08, 12 November 2007

Image:1mu8.gif

1mu8, resolution 2.0Å

Drag the structure with the mouse to rotate

thrombin-hirugen_l-378,650

Contents

Overview

Recent efforts in the field of thrombin inhibitor research have focused on, the identification of compounds with good oral bioavailability and, pharmacokinetics. In this manuscript we describe a metabolism-based, approach to the optimization of the, 3-(2-phenethylamino)-6-methylpyrazinone acetamide template (e.g., 1) which, resulted in the modification of each of the three principal components, (i.e., P1, P2, P3) comprising this series. As a result of these studies, several potent thrombin inhibitors (e.g., 20, 24, 25) were identified, which exhibit high levels of oral bioavailability and long plasma, half-lives.

Disease

Known diseases associated with this structure: Dysprothrombinemia OMIM:[176930], Hyperprothrombinemia OMIM:[176930], Hypoprothrombinemia OMIM:[176930]

About this Structure

1MU8 is a Protein complex structure of sequences from Homo sapiens with CDB as ligand. Active as Thrombin, with EC number 3.4.21.5 Full crystallographic information is available from OCA.

Reference

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines., Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, J Med Chem. 2003 Feb 13;46(4):461-73. PMID:12570369

Page seeded by OCA on Mon Nov 12 18:14:56 2007

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