AI Article Synopsis
- Researchers used Structure-Activity Relationship (SAR) data from peptide libraries to create effective deoxybenzoin inhibitors of PTP-1B.
- The addition of an ortho bromo group next to the difluoromethylphosphonate significantly boosted the potency of these compounds, achieving a 20-fold increase over the ones without the bromo substituent.
- These developed inhibitors showed good oral bioavailability and were effective in animal models studying non-insulin dependent diabetes mellitus (NIDDM).
Article Abstract
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).
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| http://dx.doi.org/10.1016/j.bmcl.2003.11.048 | DOI Listing |
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