261175-07-9Relevant academic research and scientific papers
The development of potent non-peptidic PTP-1B inhibitors
Dufresne, Claude,Roy, Patrick,Wang, Zhaoyin,Asante-Appiah, Ernest,Cromlish, Wanda,Boie, Yves,Forghani, Farnaz,Desmarais, Sylvie,Wang, Qingping,Skorey, Kathryn,Waddleton, Deena,Ramachandran, Chidambaram,Kennedy, Brian P.,Xu, Lijing,Gordon, Robert,Chan, Chi Chung,Leblanc, Yves
, p. 1039 - 1042 (2007/10/03)
The SAR from our peptide libraries was exploited to design a series of potent deoxybenzoin PTP-1B inhibitors. The introduction of an ortho bromo substituent next to the difluoromethylphosphonate warhead gave up to 20-fold increase in potency compared to the desbromo analogues. In addition, these compounds were orally bioavailable and active in the animal models of non-insulin dependent diabetes mellitus (NIDDM).
