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Discovery of 1′-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3′-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach

Colin Zhang, Meizhong Xu, Chunhong He, Jin‐Cong Zhuo, David Burns, Ding‐Quan Qian, Qiyan Lin, Yunlong Li, Lihua Chen, Eric Shi, Costas Agrios, Linkai Weng, Vaqar Sharief, Ravi Jalluri, Yanlong Li, Peggy Scherle, Sharon Diamond, Deborah Hunter, Maryanne Covington, Cindy Marando, Richard Wynn, Kamna Katiyar, Nancy Contel, Kris Vaddi, Swamy Yeleswaram, Gregory Hollis, Reid Huber, Steve Friedman, Brian Metcalf, Wenqing Yao

2022Bioorganic & Medicinal Chemistry Letters12 citationsDOIOpen Access PDF

Topics & Concepts

ChemistryPharmacophore11β-hydroxysteroid dehydrogenase type 1ScaffoldCortisoneAdipose tissuePharmacologySteroidDiabetes mellitusInsulinInternal medicineEndocrinologyEnzymeDehydrogenaseBiochemistryBiologyMedicineHormoneBiomedical engineeringHormonal Regulation and HypertensionAdrenal Hormones and DisordersPharmacogenetics and Drug Metabolism
Discovery of 1′-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3′-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach | Litcius