New 3-alkylamino-4 H-thieno-1, 2, 4-thiadiazine 1, 1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells

…, TB Bodvarsdottir, C Stidsen, A Worsaae…

Index: Nielsen, Flemming E.; Ebdrup, Sooren; Jensen, Anette Frost; Ynddal, Lars; Bodvarsdottir, Thora B.; Stidsen, Carsten; Worsaae, Anne; Boonen, Harrie C. M.; Arkhammar, Per O. G.; Fremming, Tinna; Wahl, Philip; Korno, Hanne T.; Hansen, J. Bondo Journal of Medicinal Chemistry, 2006 , vol. 49, # 14 p. 4127 - 4139

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Citation Number: 22

Abstract

Compound 1a (NN414) is a potent opener of Kir6. 2/SUR1 K ATP channels. Compound 1a inhibits insulin release in vitro and in vivo and preserves beta cell function in preclinical animal models suggesting that such a compound could find use in treatment or prevention of type 1 and type 2 diabetes. The crystal structure and a convergent synthesis of 1a are presented together with a range of new analogues of 1a. Several compounds, eg, 6- ...