title: Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).
abstract: Starting from high throughput screening hit 2-adamantyl acetic acid 3, a series of polycyclic acids have been designed and synthesized as novel, potent, and selective inhibitors of human 11β-HSD-1. Structure-activity relationships of two different regions of the chemotype (polycyclic ring and substituents on quaternary carbon) are discussed.
authors: Department of Chemistry, Research & Development, Bristol-Myers Squibb, PO Box 5400, Princeton, NJ 08543-5400, USA. xiang-yang.ye@bms.com
authors: Xiang-Yang
authors: XY
authors: Ye
authors: Stephanie Y
authors: SY
authors: Chen
authors: Akbar
authors: A
authors: Nayeem
authors: Rajasree
authors: R
authors: Golla
authors: Ramakrishna
authors: R
authors: Seethala
authors: Mengmeng
authors: M
authors: Wang
authors: Timothy
authors: T
authors: Harper
authors: Bogdan G
authors: BG
authors: Sleczka
authors: Yi-Xin
authors: YX
authors: Li
authors: Bin
authors: B
authors: He
authors: Mark
authors: M
authors: Kirby
authors: David A
authors: DA
authors: Gordon
authors: Jeffrey A
authors: JA
authors: Robl
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D019342:Acetic Acid / Q000737:chemistry / Q000494:pharmacology; D000143:Acids / Q000737:chemistry / Q000494:pharmacology*; D000218:Adamantane / Q000031:analogs & derivatives / Q000494:pharmacology*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D000143:Acids; D004791:Enzyme Inhibitors; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; C468386:HSD11B1 protein, human; D000218:Adamantane; D019342:Acetic Acid