New biologically active pregnan-21-oic acid esters. |
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| Authors: | H Laurent E Gerhards R Wiechert |
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| Affiliation: | 1. Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA;2. Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;3. Department of Chemical Research, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA;1. Department of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, via Ospedale 72, Cagliari I, 09124, Italy;2. Institute of Metabolism and Systems Research, University of Birmingham, 2nd Floor IBR Tower, Birmingham, B15 2TT, UK;3. Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, B15 2TH, UK;4. Medicinal Chemistry & Drug Discovery, Department of Pharmacology, University of Oxford, Mansfield Road, Oxford, OX1 3QT, UK;1. College of Chemistry and Pharmaceutical Sciences, Qingdao Agricultural University, Qingdao 266109, China;2. Department of Chemistry, Tsinghua University, Beijing 10084, China;1. Centre for Chemical Science & Technology, Institute of Science & Technology, JNTUH, Kukatpally, Hyderabad, 500 085, India;2. Gland Pharma Ltd, Research and Development, D.P.Pally, Hyderabad, 500 043, India |
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| Abstract: | Among the metabolites of fluocortolone (IV), isolated from human urine, there was found fluocortolone-21-acid (XI). This metabolite and several ester derivatives were synthesized by different routes starting from fluocortolone. The synthetic methods used to prepare the fluocortolone acid esters were extended to other corticoid derivatives. Several pregnan-21-oic acid esters possess the unique activity that they are topical anti-inflammatory agents with no side effects. Even when administered at high dosages, the usual systemic activity associated with corticosteroid treatment could not be observed. |
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