Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells

F. Somers, P. De Tullio, S. Boverie, J.M. Dogné, X. De Leval, M.-H. Antoine, P. Lebrun, B. Pirotte

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)89-95
Number of pages7
JournalPharmacy and pharmacology communications
Volume6
Issue number2
Publication statusPublished - 1 Feb 2000

Fingerprint

Benzothiadiazines
Insulin-Secreting Cells
Adenosine Triphosphate
Insulin

Cite this

Somers, F. ; De Tullio, P. ; Boverie, S. ; Dogné, J.M. ; De Leval, X. ; Antoine, M.-H. ; Lebrun, P. ; Pirotte, B. / Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells. In: Pharmacy and pharmacology communications. 2000 ; Vol. 6, No. 2. pp. 89-95.
@article{98be6e056ac74ab88b99bda037ec5e0e,
title = "Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells",
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.",
author = "F. Somers and {De Tullio}, P. and S. Boverie and J.M. Dogn{\'e} and {De Leval}, X. and M.-H. Antoine and P. Lebrun and B. Pirotte",
year = "2000",
month = "2",
day = "1",
language = "English",
volume = "6",
pages = "89--95",
journal = "Pharmacy and pharmacology communications",
issn = "1460-8081",
publisher = "Pharmaceutical Press",
number = "2",

}

Somers, F, De Tullio, P, Boverie, S, Dogné, JM, De Leval, X, Antoine, M-H, Lebrun, P & Pirotte, B 2000, 'Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells', Pharmacy and pharmacology communications, vol. 6, no. 2, pp. 89-95.

Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells. / Somers, F.; De Tullio, P.; Boverie, S.; Dogné, J.M.; De Leval, X.; Antoine, M.-H.; Lebrun, P.; Pirotte, B.

In: Pharmacy and pharmacology communications, Vol. 6, No. 2, 01.02.2000, p. 89-95.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Synthesis and biological effects of new 3-alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides on insulin-secreting cells

AU - Somers, F.

AU - De Tullio, P.

AU - Boverie, S.

AU - Dogné, J.M.

AU - De Leval, X.

AU - Antoine, M.-H.

AU - Lebrun, P.

AU - Pirotte, B.

PY - 2000/2/1

Y1 - 2000/2/1

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0034111292&partnerID=8YFLogxK

M3 - Article

AN - SCOPUS:0034111292

VL - 6

SP - 89

EP - 95

JO - Pharmacy and pharmacology communications

JF - Pharmacy and pharmacology communications

SN - 1460-8081

IS - 2

ER -