Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 2. Syntheses and biological activities of 1, 4-dialkyl-, …

G Le Bihan, F Rondu, A Pelé-Tounian…

Index: Le Bihan, Gaelle; Rondu, Frederic; Pele-Tounian, Agnes; Wang, Xuan; Lidy, Sandrine; Touboul, Estera; Lamouri, Aazdine; Dive, Georges; Huet, Jack; Pfeiffer, Bruno; Renard, Pierre; Guardiola-Lemaitre, Beatrice; Manechez, Dominique; Penicaud, Luc; Ktorza, Alain; Godfroid, Jean-Jacques Journal of Medicinal Chemistry, 1999 , vol. 42, # 9 p. 1587 - 1603

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Citation Number: 66

Abstract

Piperazine derivatives have been identified as new antidiabetic compounds. Structure- activity relationship studies in a series of 1-benzyl-4-alkyl-2-(4', 5'-dihydro-1'H-imidazol-2'-yl) piperazines resulted in the identification of 1-methyl-4-(2', 4'-dichlorobenzyl)-2-(4', 5'-dihydro- 1'H-imidazol-2'-yl) piperazine, PMS 812 (S-21663), as a highly potent antidiabetic agent on a rat model of diabetes, mediated by an important increase of insulin secretion ...