Synthesis of a series of imidazolines with glucose dependent effects on insulin exocytosis from pancreatic β-cells is reported. Regioisomers and enantiomers were found to exhibit marked differences in exocytotic effects as well as different activities on the KATP-channel; the (R (+)) isomer of 2-[2-(4, 5-dihydro-1H-imidazol-2-yl)-1-thiophene-2-ylethyl] pyridine (4a) and the (+) isomer of 2-[2-(4, 5-dihydro-1H-imidazol-2-yl)-1-thiophene-3-ylethyl] pyridine ( ...
