SYNTHETIC STUDIES OF VITAMIN-D ANALOGS .24. SYNTHESIS OF ACTIVE VITAMIN-D-3 ANALOGS SUBSTITUTED AT THE 2-BETA-POSITION AND THEIR PREVENTIVEEFFECTS ON BONE-MINERAL LOSS IN OVARIECTOMIZED RATS
Y. Ono et al., SYNTHETIC STUDIES OF VITAMIN-D ANALOGS .24. SYNTHESIS OF ACTIVE VITAMIN-D-3 ANALOGS SUBSTITUTED AT THE 2-BETA-POSITION AND THEIR PREVENTIVEEFFECTS ON BONE-MINERAL LOSS IN OVARIECTOMIZED RATS, Chemical and Pharmaceutical Bulletin, 45(10), 1997, pp. 1626-1630
Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitam
in D-3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D-3 bea
ring substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitami
n D-3 (1), were synthesized from the alpha-epoxides (6 and 13), Three
analogs, ED-71 (4) and two carba-type analogs (16 acid 26), showed pot
ent preventive effects on bone mineral loss in pre-osteoporosis model
rats, ED-71 (4) was concluded to be an optimized analog and a promisin
g candidate for the treatment of osteoporosis.