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• W3022011014 abstract "Abstract TAK‐875 (compound 1 ) was the only GPR40 agonist with promising oral glucose‐lowering effect, which entered phase III clinical trials. In previous studies, we successfully synthesized the TAK‐875 sulfoxide analog 2 , which was further separated to optically pure compounds 3 (S, S, 100.0% de) and 4 (R, S, 100.0% de). In vitro biological evaluation revealed that the sulfoxide analogs 3 and 4 possessed comparable GPR40 agonist activity to TAK‐875. Herein, in order to further evaluate the druglikeness of TAK‐875 sulfoxide analogs, the pharmacokinetic properties of compounds 2 , 3 , and 4 in rats were investigated and compared with that of TAK‐875. The results showed that sulfoxide ( 2 , 3 , and 4 ) and sulfone (TAK‐875) could be converted into each other in different degrees in vivo. Interestingly, compound 3 showed higher drug exposure calculated by the AUC sum of sulfoxide and sulfone in plasma than TAK‐875, 2 and 4 . In order to further investigate the in vivo glucose‐lowering potency of sulfoxide analogs, asymmetric synthesis was carried out and led to two sulfoxides with moderate de values, 5 (S, S, 66.4% de) and 6 (R, S, 71.0% de). The following oral glucose tolerance test (OGTT) in rats showed that 5 (S, S, 66.4% de) had stronger glucose‐lowering effect in vivo than 6 (R, S, 71.0% de) and TAK‐875, which could be partly rationalized by the superior pharmacokinetic property of sulfoxide 3 (the main component of 5 ) relative to sulfoxide 4 (the main component of 6 ) and TAK‐875." @default.
• W3022011014 created "2020-05-13" @default.
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• W3022011014 date "2020-05-02" @default.
• W3022011014 modified "2023-10-18" @default.
• W3022011014 title "In vivo pharmacokinetic study and oral glucose tolerance test of sulfoxide analogs of <scp>GPR40</scp> agonist <scp>TAK</scp> ‐875" @default.
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• W3022011014 doi "https://doi.org/10.1002/ddr.21675" @default.
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