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Bioorg Med Chem Lett. 2004 Jul 16;14(14):3775-9.

Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.

Author information

1
Pharmaceutical Technology Institute, Otsuka Pharmaceutical Factory, Inc. Tateiwa, Muya-cho, Naruto, Tokushima 772-8601, Japan. okamurtk@otsukakj.co.jp

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.

PMID:
15203160
DOI:
10.1016/j.bmcl.2004.04.099
[Indexed for MEDLINE]

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