AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey
| Autor: | Raymond E. Conrow, Mark R. Hellberg, David Earnest, Gary W. Williams, Pete Delgado, W. Dennis Dean, Najam A. Sharif, Peter G. Klimko, Michael S. Gaines, Karen S. Haggard, Robert D. Selliah, Marsha A. McLaughlin, Daniel Scott |
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| Rok vydání: | 2004 |
| Předmět: |
Agonist
medicine.medical_specialty medicine.drug_class Administration Topical Clinical Biochemistry Pharmaceutical Science Prostaglandin Ocular Hypotension Biochemistry Chemical synthesis chemistry.chemical_compound Internal medicine Drug Discovery medicine Animals Molecular Biology Lagomorpha biology Chemistry Organic Chemistry Biological activity Haplorhini Prodrug biology.organism_classification Endocrinology Prostaglandin analog Cats Prostaglandins Molecular Medicine Rabbits Isopropyl |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:4525-4528 |
| ISSN: | 0960-894X |
| Popis: | A series of 11-oxa prostaglandin analogs was evaluated for FP receptor binding and activation. Several compounds having aryloxy-terminated lower chains were found to be potent agonists. Topical ocular dosing of AL-12182, the isopropyl ester prodrug of the potent agonist 13, lowered intraocular pressure in the monkey by 40% accompanied by minimal conjunctival hyperemia in the rabbit. AL-12182 was synthesized on multigram scale starting with D-sorbitol. |
| Databáze: | OpenAIRE |
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