The universal template approach provided a prospect of modifying methoctramine (2) structure. Thus, polyamines 3-7 were designed in which the flexibility of the diaminohexane spacer of 2 was replaced by a bipiperidinyl moiety. In electrically stimulated guinea pig left atria, these novel polyamines, unlike prototype 2, displayed a potent intrinsic activity, which was in contrast with the muscarinic antagonism shown in binding studies by some of them (3 and 4) and was inhibited by benzalkonium chloride, an inhibitor of Gi proteins.
Melchiorre C., Bolognesi M.L., Budriesi R., Ghelardini C., Chiarini A., Minarini A., et al. (2001). Design, synthesis, and biological activity of methoctramine-related polyamines as putative Gi protein activators. JOURNAL OF MEDICINAL CHEMISTRY, 44(24), 4035-4038 [10.1021/jm0155594].
Design, synthesis, and biological activity of methoctramine-related polyamines as putative Gi protein activators
Melchiorre C.;Bolognesi M. L.;Budriesi R.;Chiarini A.;Minarini A.;Rosini M.;Tumiatti V.;
2001
Abstract
The universal template approach provided a prospect of modifying methoctramine (2) structure. Thus, polyamines 3-7 were designed in which the flexibility of the diaminohexane spacer of 2 was replaced by a bipiperidinyl moiety. In electrically stimulated guinea pig left atria, these novel polyamines, unlike prototype 2, displayed a potent intrinsic activity, which was in contrast with the muscarinic antagonism shown in binding studies by some of them (3 and 4) and was inhibited by benzalkonium chloride, an inhibitor of Gi proteins.| File | Dimensione | Formato | |
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J. Med. Chem. 2001, 44, 24, 4035–4038.pdf
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