Abstract
3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides with nitro, amino or acetylamino groups in the 7-position have been synthesized in an attempt to discover new tissue-selective K(ATP)-channel openers. The compounds were tested as putative pancreatic β-cells K(ATP)-channel openers by measuring their inhibitory activity on the insulin releasing process. The influence of the substituent in the 7-position on the acidic character (pK(a)) and on biological activity is discussed. The nitrobenzene derivatives were biologically active, but less so than the un-derivatized parent pyridothiadiazine dioxides.
Original language | English |
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Pages (from-to) | 89-95 |
Number of pages | 7 |
Journal | Pharmacy and pharmacology communications |
Volume | 6 |
Issue number | 2 |
Publication status | Published - 1 Feb 2000 |