calpain and pyridine

calpain has been researched along with pyridine* in 1 studies

Other Studies

1 other study(ies) available for calpain and pyridine

Article	Year
Exploration of orally available calpain inhibitors. Part 3: Dipeptidyl alpha-ketoamide derivatives containing pyridine moiety. Bioorganic & medicinal chemistry, 2006, Aug-15, Volume: 14, Issue:16 Calpain-mediated proteolysis has been implicated as a major process in neuronal cell death including retinal neurological degeneration. The previously reported calpain inhibitor SJA6017 (1) showed oral efficacy in a retinal pharmacological model, but its oral bioavailability was low due to the metabolic lability and low water-solubility. The purpose of present study was to identify good orally bioavailable calpain inhibitors. A series of water-soluble dipeptidyl alpha-ketoamides containing a pyridine moiety at P3 were designed, synthesized, and evaluated for their oral bioavailability and retinal penetration. Introduction of a pyridineethanol moiety provided the potent alpha-ketoamide inhibitor 8 with good oral bioavailability. Compound 8 showed about 12-fold higher retinal AUC than 1. Topics: Administration, Oral; Animals; Biological Availability; Calpain; Cell Death; Dipeptides; Humans; Neuroprotective Agents; Pyridines; Rats; Rats, Sprague-Dawley; Retinal Degeneration; Solubility; Structure-Activity Relationship; Water	2006

Article

Year

Exploration of orally available calpain inhibitors. Part 3: Dipeptidyl alpha-ketoamide derivatives containing pyridine moiety.

Bioorganic & medicinal chemistry, 2006, Aug-15, Volume: 14, Issue:16

Calpain-mediated proteolysis has been implicated as a major process in neuronal cell death including retinal neurological degeneration. The previously reported calpain inhibitor SJA6017 (1) showed oral efficacy in a retinal pharmacological model, but its oral bioavailability was low due to the metabolic lability and low water-solubility. The purpose of present study was to identify good orally bioavailable calpain inhibitors. A series of water-soluble dipeptidyl alpha-ketoamides containing a pyridine moiety at P3 were designed, synthesized, and evaluated for their oral bioavailability and retinal penetration. Introduction of a pyridineethanol moiety provided the potent alpha-ketoamide inhibitor 8 with good oral bioavailability. Compound 8 showed about 12-fold higher retinal AUC than 1.

Topics: Administration, Oral; Animals; Biological Availability; Calpain; Cell Death; Dipeptides; Humans; Neuroprotective Agents; Pyridines; Rats; Rats, Sprague-Dawley; Retinal Degeneration; Solubility; Structure-Activity Relationship; Water

2006