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2005
Pyrazine derivatives
R 0550
Synthesis and Pharmacological Evaluation of Substituted 5-[4-[2-(6,7-Dimeth25- 156 yl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylenethiazolidine-2,4-dione Derivatives as Potent Euglycemic and Hypolipidemic Agents. —
Title derivatives (V) are prepared by Knoevenagel condensation of condensation product (III) with thiazolidinedione (IV) in the presence of a catalytic amount of piperidinium benzoate and azeotropic removal of water. Derivatives (V) display a notable decrease in glucose and triglyceride level. In general, compounds having other than hydrogen or methyl substituents at C-3 of the tetrahydroquinoxalinone moiety as well as
a shorter CH2 spacer show lower euglycemic and hypolipidemic activities. Based on in
vivo data, (Va) is identified as a potent euglycemic and hypolipidemic agent (no yields
given). — (GUPTA, D.; GHOSH, N. N.; CHANDRA*, R.; Bioorg. Med. Chem. Lett.
15 (2005) 4, 1019-1022; Ambedkar Cent. Biomed. Res., Univ. Delhi, Delhi 110 007,
India; Eng.) — H. Hoennerscheid
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