Synthesis of 21-nor-22-oxa-1α,25-dihydroxyvitamin D3 derivatives in quest of a drug with low calcemic activity |
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Authors: | Hitoshi Shimizu Kazuki Shimizu Atsuko Sugita Tsuyoshi Yamauchi Kazumi Morikawa |
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Institution: | a Synthetic Technology Research Department, Chugai Pharmaceutical Co., Ltd, 5-5-1 Ukima, Kita-Ku, Tokyo 115-8543, Japan b Chemistry Research Department I and Pharmaceutical Research Department II, Chugai Pharmaceutical Co., Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan |
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Abstract: | Two 21-nor-22-oxa-1α,25-dihydroxyvitamin D3 derivatives have been synthesized in quest of a drug with lower calcemic activity than Maxacalcitol, 22-oxa-1α,25-dihydroxyvitamin D3, being used as antihyperparathyroidism and antipsoriatic drug. Of two 21-nor products obtained, the product carrying one carbon elongated side chain with diethylcarbinol moiety has been found to exhibit comparable differentiation-inducing activity to Maxacalcitol with much lower exhibition of calcemic activity. |
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Keywords: | Vitamin D3 derivative 22-Oxavitamin D3 derivatives Separation of activity Calcemic activity Differentiation-inducing activity |
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