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Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy |
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| Authors: | Thompson Christopher F Quraishi Nazia Ali Amjad Tata James R Hammond Milton L Balkovec James M Einstein Monica Ge Lan Harris Georgianna Kelly Theresa M Mazur Paul Pandit Shilpa Santoro Joseph Sitlani Ayesha Wang Chuanlin Williamson Joanne Miller Douglas K Yamin Ting-ting D Thompson Chris M O'Neill Edward A Zaller Dennis Forrest Michael J Carballo-Jane Ester Luell Silvi |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christopher_thompson@merck.com |
| Abstract: | A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse. |
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