La. Reiter et al., 3-SUBSTITUTED-4-HYDROXY-7-CHROMANYLACETIC ACID-DERIVATIVES AS ANTAGONISTS OF THE LEUKOTRIENE B-4 (LTB4) RECEPTOR, Bioorganic & medicinal chemistry letters, 7(17), 1997, pp. 2307-2312
The SAR of a series of 7-chromanylacetic acids has been investigated w
ith the aim of identifying potent and selective LTB4 receptor antagoni
sts. We found optimal activity in derivatives with alpha,alpha-disubst
itution on the acetic acid and a C-4 hydroxy group and a C-3 lipophili
c group on the chromane ring. CP-105696 (43), which contains a 4-pheny
lbenzyl C-3 substituent, was selected for development. (C) 1997 Elsevi
er Science Ltd.