Abstract
Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitamin D3 (1), were synthesized from the alpha-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.
MeSH terms
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Absorptiometry, Photon
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Animals
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Bone Density / drug effects*
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Calcitriol / analogs & derivatives*
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Calcitriol / chemistry
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Calcitriol / pharmacology
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Cholecalciferol / analogs & derivatives*
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Cholecalciferol / pharmacology*
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Disease Models, Animal
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Drug Design
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Female
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Humans
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Osteoporosis, Postmenopausal / prevention & control*
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Ovariectomy
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Rats
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Rats, Wistar
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Receptors, Calcitriol / drug effects
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Receptors, Calcitriol / metabolism
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Vitamin D / analogs & derivatives
Substances
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Receptors, Calcitriol
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Vitamin D
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Cholecalciferol
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Calcitriol
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eldecalcitol