title: Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.
abstract: In order to investigate SAR regarding proximal phenyl ring in novel C-aryl glucoside SGLT2 inhibitors containing a thiazole motif, a series of chemical modifications on proximal phenyl ring was conducted. During a series of lead optimization efforts, ortho-allyloxyphenyl 10p or ortho-hydroxyphenyl 11a showed subnanomolar inhibitory activity against hSGLT2.
authors.affiliation: Green Cross Corporation Research Center, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
authors.forename: Suk Ho
authors.initials: SH
authors.lastname: Lee
authors.forename: Min Ju
authors.initials: MJ
authors.lastname: Kim
authors.forename: Sung-Han
authors.initials: SH
authors.lastname: Lee
authors.forename: Jeongmin
authors.initials: J
authors.lastname: Kim
authors.forename: Hyun-Ju
authors.initials: HJ
authors.lastname: Park
authors.forename: Jinhwa
authors.initials: J
authors.lastname: Lee
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D016466:CHO Cells; D002250:Carbon Radioisotopes; D003412:Cricetulus; D015870:Gene Expression; D005960:Glucosides / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008757:Methylglucosides / Q000378:metabolism; D011994:Recombinant Proteins / Q000737:chemistry; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000494:pharmacology; D051297:Sodium-Glucose Transporter 2 / Q000737:chemistry; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002250:Carbon Radioisotopes; D005960:Glucosides; D007004:Hypoglycemic Agents; D008757:Methylglucosides; D011994:Recombinant Proteins; C089180:SLC5A2 protein, human; D054852:Small Molecule Libraries; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013844:Thiazoles