Alexander Macdonald

Small-volume solid-elcetrode flow-through electrochemical cells : Preliminary evaluation using pulse polarographic techniques

Abstract A preliminary evaluation is given of the use of potentiostatic pulse polarographic techniques for solid-electrode flow-through electrochemical cells as detectors for use in both automated analysis and liquid chromatography. The following advanatages are noted over previously reported constant-applied-potential techniques: increased sensitivity, minimal effect of flow-rate on current measurement and a vast increase in electrode stability for the short-term sampling period and for extended routing operation.

Discovery of carmegliptin: A potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the enzyme and early efficacy data in animal models of type 2 diabetes are also presented.