title: Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors.
abstract: Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1.
authors.affiliation: Amgen Inc., South San Francisco, CA 94080, USA. xdu@amgen.com
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Du
authors.forename: Mike
authors.initials: M
authors.lastname: Lizarzaburu
authors.forename: Simon
authors.initials: S
authors.lastname: Turcotte
authors.forename: Taeweon
authors.initials: T
authors.lastname: Lee
authors.forename: Joanne
authors.initials: J
authors.lastname: Greenberg
authors.forename: Bei
authors.initials: B
authors.lastname: Shan
authors.forename: Peter
authors.initials: P
authors.lastname: Fan
authors.forename: Yun
authors.initials: Y
authors.lastname: Ling
authors.forename: Julio C
authors.initials: JC
authors.lastname: Medina
authors.forename: Jonathan
authors.initials: J
authors.lastname: Houze
mesh_terms: D004355:Drug Stability; D015394:Molecular Structure; D010695:Phlorhizin / Q000737:chemistry; D012995:Solubility; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D014230:Triazoles; D010695:Phlorhizin