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Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors |
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| Authors: | Du Xiaohui Lizarzaburu Mike Turcotte Simon Lee Taeweon Greenberg Joanne Shan Bei Fan Peter Ling Yun Medina Julio C Houze Jonathan |
| Institution: | Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA |
| 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 |
| Keywords: | Noncompetitive SGLT2 inhibitors Triazoles SAR Solubility Benzooxazinone head groups Indane tail group |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |