Bioorganic & Medicinal Chemistry 2009-01-01

Discovery of 13-oxa prostaglandin analogs as antiglaucoma agents: Synthesis and biological activity

Zixia Feng, Mark R. Hellberg, Najam A. Sharif, Marsha A. McLaughlin, Gary W. Williams, Daniel Scott, Tony Wallace, Zixia Feng, Mark R. Hellberg, Najam A. Sharif, Marsha A. McLaughlin, Gary W. Williams, Daniel Scott, Tony Wallace

Index: Bioorg. Med. Chem. 17 , 576-84, (2009)

Full Text: HTML

Abstract

Novel 13-oxa prostaglandin analogs were designed, synthesized and evaluated for their antiglaucoma activities. AL-16082 was the most potent prostaglandin FP agonist in vitro (EC 50 = 1.9 nM). Its pro-drug AL-16049 significantly lowered intraocular pressure in the ocular hypertensive monkey eyes by 30% with low side-effects.