Imidazolines as efficacious glucose-dependent stimulators of insulin secretion

P Jakobsen, P Madsen, HS Andersen

Index: Jakobsen, Palle; Madsen, Peter; Andersen, HenrikSune European Journal of Medicinal Chemistry, 2003 , vol. 38, # 4 p. 357 - 362

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Citation Number: 8

Abstract

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 ( ...