Molecular design to enhance the penetration into the retina via ocular instillation
| Autor: | Masazumi Yamaguchi, Hiroaki Takahashi, Yoshihisa Shirasaki, Jun Inoue |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
genetic structures
Clinical Biochemistry Pharmaceutical Science Administration Oral Biochemistry Retina chemistry.chemical_compound Structure-Activity Relationship Pharmacokinetics Oral administration Drug Discovery medicine Animals Humans Enzyme Inhibitors Molecular Biology biology Molecular Structure Calpain Organic Chemistry Retinal Penetration (firestop) eye diseases Macaca fascicularis medicine.anatomical_structure chemistry Enzyme inhibitor Drug Design Lipophilicity Injections Intravenous biology.protein Biophysics Molecular Medicine sense organs Carbamates Rabbits |
| Zdroj: | Bioorganicmedicinal chemistry letters. 18(19) |
| ISSN: | 1464-3405 |
| Popis: | To investigate the molecular design of drugs that have good penetration into the retina from anterior segment of the eye via ocular instillation, we optimized the length of methoxyethylene glycol chain (mEG) in the P3 region of an oral bioavailable calpain inhibitor SNJ-1945 (2) as a model compound. Modulation of the mEG length led to the optimal balance between hydrophilicity and lipophilicity and provided the compound with higher retinal exposure via ocular instillation. Incorporation of a mEG moiety would be a useful and convenient approach to attain high intraocular penetration. |
| Databáze: | OpenAIRE |
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