Peer-reviewed veterinary case report
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2004
- Authors:
- Okamura, Takashi et al.
- Affiliation:
- Pharmaceutical Technology Institute · Japan
Abstract
Structure-activity relationships (SAR) of fused 1,2,4-triazolo[1,5-c ]pyrimidine were performed. Various substituents were introduced into the heterocyclic ring to improve the potency of adenosine A(3) receptor binding affinity and A(3)-selectivity against other subtypes. Potent and selective A(3) receptor antagonists were identified and were evaluated in a monkey model of intraocular pressure by eye-drop administration. As a result, compound 1c (OT-7999) was found to significantly decrease intraocular pressure in the animal model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15203160/