1997 Volume 45 Issue 10 Pages 1626-1630
Analogs related to 1α, 25-dihydroxy-2β-(3-hydroxypropoxy)vitamin D3 (ED-71)(4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2β-position of 1α, 25-dihydroxyvitamin D3 (1), were synthesized from the α-epoxides (6 and 13). Three analogs, ED-71 (4) and two carba-type analogs (16 and 26), showed potent preventive effects on bone mineral loss in pre-osteoporosis model rats. ED-71 (4) was concluded to be an optimized analog and a promising candidate for the treatment of osteoporosis.