- Syntheses of fluorinated ligands to probe binding of antigenic determinants of Vibrio cholerae O:1, serotypes Inaba and Ogawa, to antibodies
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Derivatives of methyl α-glycosides of antigenic determinants of Vibrio cholerae O:1, serotypes Inaba and Ogawa, specifically fluorinated at position 2' or 4' have been synthesized by coupling the appropriately fluorinated derivatives of 3-deoxy-L-glycero-tetronic acid with the methyl α-glycosides of perosamine. The compound having the fluorine atom at position 2 was obtained by electrophilic addition of fluorine to the glycal derived from the parent antigenic determinant, serotypes Inaba, using Selectfluor((TM)) as a fluorination reagent. Copyright (C) 2000 Elsevier Science Ltd.
- Chang, Alex H.C.,Horton, Derek,Kovac, Pavol
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- Synthesis of 1α,25-dihydroxy-24R-fluorocholecalciferol and 1α,25-dihydroxy-24S-fluorocholecalciferol
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1α,25-Dihydroxy-24R-fluorocholecalciferol and 1α,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1α,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D 3, are synthesized in a multistep process from the known substance 1α,3β-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1α,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies. Exemplary of such disease states are the following: osteomalacia, osteoporosis, rickets, osteitis fibrosa cystica, renal osteodystrophy, osteosclerosis, anti-convulsant treatment, osteopenia, fibrogenesis-imperfecta ossium, secondary hyperparathyrodism, hypoparathyroidism, hyperparathyroidism, cirrhosis, obstructive jaundice, drug induced metabolism, medullary carcinoma, chronic renal disease, hypophosphatemic VDRR, vitamin D-dependent rickets, sarcoidosis, glucocorticoid antagonism, malabsorption syndrome, steatorrhea, tropical sprue, idiopathic hypercalcemia and milk fever.
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- Synthesis of 1α,25-dihydroxy-24R-fluorocholecalciferol and 1α,25-dihydroxy-24S-fluorocholecalciferol
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1α,25-Dihydroxy-24R-fluorocholecalciferol and 1α,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1α,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D3, are synthesized in a multistep process from the known substance 1α,3β-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1α,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies. Exemplary of such disease states are the following: osteosclerosis, anticonvulsant treatment, osteopenia, fibrogenesis-imperfecta ossium, secondary hyperparathyrodism, hypoparathyroidism, hyperparathyroidism, cirrhosis, obstructive jaundice, drug induced metabolism, medullary carcinoma, chronic renal disease, hypophosphatemic VDRR, vitamin D-dependent rickets, sarcoidosis, glucocorticoid antagonism, malabsorption syndrome, steatorrhea, tropical sprue, idiopathic hypercalcemia and milk fever.
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