New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of “THIQ”

…, A Yahorau, E Liepinsh, S Kopantshuk…

Index: Mutulis, Felikss; Yahorava, Sviatlana; Mutule, Ilze; Yahorau, Aleh; Liepinsh, Edvards; Kopantshuk, Sergei; Veiksina, Santa; Tars, Kaspars; Belyakov, Sergey; Mishnev, Anatoly; Rinken, Ago; Wikberg, Jarl E. S. Journal of Medicinal Chemistry, 2004 , vol. 47, # 18 p. 4613 - 4626

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Citation Number: 29

Abstract

A series of piperazine analogues of the melanocortin 4 receptor (MC4R) specific small- molecule agonist “THIQ” was synthesized and characterized structurally and pharmacologically. First, several THIQ imitations lacking the triazole moiety were prepared. Syntheses included acylation of 4-phenylpiperazine or 4-cyclohexylpiperazine. In two cases the tertiary amine function was replaced by the corresponding N-oxide. To obtain more ...