title: [SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors].
abstract: Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
authors.forename: Wen-Wen
authors.initials: WW
authors.lastname: Yin
authors.forename: Zheng
authors.initials: Z
authors.lastname: Chen
authors.forename: Yan-Bo
authors.initials: YB
authors.lastname: Tang
authors.forename: Fei
authors.initials: F
authors.lastname: Ye
authors.forename: Jin-Ying
authors.initials: JY
authors.lastname: Tian
authors.forename: Zhi-Yan
authors.initials: ZY
authors.lastname: Xiao
mesh_terms: D006801:Humans; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000077589:Sulfathiazole; D013432:Sulfathiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D013432:Sulfathiazoles; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D000077589:Sulfathiazole