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ID: ALA1134916

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.

Authors: Peat AJ, Townsend C, Worley JF, Allen SH, Garrido D, Mertz RJ, Pfohl JL, Terry CM, Truax JF, Veasey RL, Thomson SA.

Abstract: A series of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives has been synthesized and evaluated as K(ATP) channel agonists using the inside-out excised patch clamp technique. The most active compounds were approximately 20-fold more potent than diazoxide in opening K(ATP) channels. A linear relationship exists between the potency of the compound and the sigma value of the 7-substituent with electron-withdrawing groups exhibiting higher activity. These compounds may be useful in modulating insulin release from pancreatic beta-cells and in diseases associated with hyperinsulinemia.

CiteXplore: 12270187

DOI: 10.1016/s0960-894x(02)00617-0