| Literature DB >> 15203160 |
Takashi Okamura1, Yasuhisa Kurogi, Kinji Hashimoto, Seiji Sato, Hiroshi Nishikawa, Kimio Kiryu, Yoshimitsu Nagao.
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.Entities:
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Year: 2004 PMID： 15203160 DOI： 10.1016/j.bmcl.2004.04.099
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823